3.1.3.48 ((1E)-2-nitroprop-1-en-1-yl)benzene 50% inhibition at 0.023 mM in absence of 2-mercaptoethanol, at 0.515 mM in presence of 1 mM 2-mercaptoethanol 129281 3.1.3.48 ((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate 50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F 129715 3.1.3.48 ((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate 50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F 129709 3.1.3.48 ((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate) 50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F 129711 3.1.3.48 ((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate 50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F 129710 3.1.3.48 ((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate 50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F 129712 3.1.3.48 ((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate 50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F 129713 3.1.3.48 ((4-((4E)-2-(1H-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonic acid 50% inhibition at 109 nM for isoform PTP-1B, at 95 nM for isoform TCPTP 129699 3.1.3.48 ((E)-2-nitrovinyl)benzene i.e. trans-beta-nitrostyrene, slow-binding inhibitor, acting as a pY mimetic and binding to the enzyme active site to form an initial noncovalent E*I complex, followed by nucleophilic attack on the nitrostyrene nitro group by C215 of enzyme to form a reversible, covalent adduct. 50% inhibition at 0.0025 mM in absence of 2-mercaptoethanol, at 0.4 mM in presence of 1 mM 2-mercaptoethanol 129277 3.1.3.48 (1-benzyl-3-methyl-2,3-dihydro-1H-imidazol-2-yl)(chloro)gold i.e. [(BzMeIm)AuICl] 158944 3.1.3.48 (1R,3aS,3bS,10aR,10bS,12aR)-1-[(2R)-4-carboxybutan-2-yl]-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-9-carboxylic acid - 197256 3.1.3.48 (1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate no inhibition at 0.021 mM 230594 3.1.3.48 (1S,3aR,8S,8aS,8bR)-4-henicosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,5a,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione - 197183 3.1.3.48 (1S,3aS,4R,8S,8aS,8bR)-4-icosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,4,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione - 197182 3.1.3.48 (2alpha,3alpha)-2,3-dihydroxyolean-12-en-28-oic acid - 68343 3.1.3.48 (2aS,3R,6aR,7aS,7bR,7cS)-2a-(hydroxymethyl)-3-icosyl-6a,7a-dimethyl-2a,3,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2,5-dione - 197187 3.1.3.48 (2aS,3R,6aR,7aS,7bR,7cS)-3-icosyl-6a,7a-dimethyl-2,5-dioxo-3,5,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2a(2H)-carbaldehyde - 197186 3.1.3.48 (2beta,3beta)-2,3-dihydroxyolean-12-en-28-oic acid - 68344 3.1.3.48 (2E)-1-(2'-hydroxyphenyl)-3-(1-naphthyl)-2-propen-1-one 76% inhibition at 0.025 mM 79063 3.1.3.48 (2E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 79270 3.1.3.48 (2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one 20% inhibition at 0.025 mM 158929 3.1.3.48 (2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one - 158930 3.1.3.48 (2E)-1-(2,5-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one 58% inhibition at 0.025 mM 79180 3.1.3.48 (2E)-1-(2,5-dimethoxyphenyl)-3-(naphth-1-yl)-2-propen-1-one 46% inhibition at 0.025 mM 78968 3.1.3.48 (2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one 8% inhibition at 0.025 mM 158927 3.1.3.48 (2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one 16% inhibition at 0.025 mM 158928 3.1.3.48 (2E)-1-(2-hydroxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one 26% inhibition at 0.025 mM 158996 3.1.3.48 (2E)-1-(3,4-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one - 79156 3.1.3.48 (2E)-1-(3,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one 68.5% inhibition at 0.025 mM 158920 3.1.3.48 (2E)-1-(3-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one - 85226 3.1.3.48 (2E)-1-(3-hydroxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one 20% inhibition at 0.025 mM 158973 3.1.3.48 (2E)-1-(3-methoxy-4-hydroxyphenyl)-3-(2-naphthyl)-2-propen-1-one - 79214 3.1.3.48 (2E)-1-(3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one 18.5% inhibition at 0.025 mM 158925 3.1.3.48 (2E)-1-(4-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one - 85225 3.1.3.48 (2E)-1-(4-bromophenyl)-3-(naphthalen-1-yl)prop-2-en-1-one 25% inhibition at 0.025 mM 158923 3.1.3.48 (2E)-1-(4-bromophenyl)-3-(naphthalen-2-yl)prop-2-en-1-one 11% inhibition at 0.025 mM 158924 3.1.3.48 (2E)-1-(4-hydroxy-3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one 39% inhibition at 0.025 mM 158991 3.1.3.48 (2E)-1-(4-methoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one 18% inhibition at 0.025 mM 158910 3.1.3.48 (2E)-1-[3-(benzyloxy)phenyl]-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one - 85215 3.1.3.48 (2E)-2-[1-carbamothioyl-3-(4-nitrophenyl)-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]-1-(4-sulfophenyl)diazanide - 197235 3.1.3.48 (2E)-2-[[5-(3-carboxy-4-hydroxycyclohexa-1,5-dien-1-yl)furan-2-yl]methylidene]-1-[6-[(4-fluorophenyl)amino][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]diazanide - 197225 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(2,4-dimethoxyphenyl)prop-2-en-1-one 8% inhibition at 0.025 mM 158984 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(2,5-dimethoxyphenyl)prop-2-en-1-one 9% inhibition at 0.025 mM 158851 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one - 18875 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one 18% inhibition at 0.025 mM 158913 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one - 158914 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(3-nitrophenyl)prop-2-en-1-one 26% inhibition at 0.025 mM 158912 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one 14% inhibition at 0.025 mM 40282 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(4-hydroxy-3-methoxyphenyl)prop-2-en-1-one 20% inhibition at 0.025 mM 158887 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(4-methoxyphenyl)prop-2-en-1-one 6% inhibition at 0.025 mM 158905 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-(4-nitrophenyl)prop-2-en-1-one 19.5% inhibition at 0.025 mM 158906 3.1.3.48 (2E)-3-(1,3-benzodioxol-5-yl)-1-phenylprop-2-en-1-one - 158994 3.1.3.48 (2E)-3-(3,4-dichlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one - 158904 3.1.3.48 (2E)-3-(3-chlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one - 158907 3.1.3.48 (2E)-3-(3-chlorophenyl)-1-(2-hydroxy-4,6-dimethoxyphenyl)prop-2-en-1-one 13% inhibition at 0.025 mM 158908 3.1.3.48 (2E)-3-(3-nitrophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one - 158810 3.1.3.48 (2E)-3-(4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 79142 3.1.3.48 (2E)-3-(5-bromo-2,4-dihydroxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one - 85248 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one - 85213 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-[[(methoxycarbonyl)sulfanyl]amino]phenyl)prop-2-en-1-one - 85239 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-butoxyphenyl)prop-2-en-1-one - 85214 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one - 85211 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one - 85212 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one - 85228 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one - 85235 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one - 85232 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(3-methylbut-3-en-2-yl)-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one - 85247 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one - 85229 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one - 85236 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one - 85233 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(1H-pyrazol-1-yl)phenyl]prop-2-en-1-one - 85237 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one - 85227 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(methylsulfonyl)phenyl]prop-2-en-1-one - 85224 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one - 85238 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one - 85234 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one - 85242 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one - 85243 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one - 85241 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one - 85245 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one - 85246 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one - 85244 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one - 15183 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(4-methylphenyl)sulfonyl]phenyl]prop-2-en-1-one - 85223 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one - 85231 3.1.3.48 (2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)-1,3-benzodioxol-5-yl]prop-2-en-1-one - 85230 3.1.3.48 (2E)-3-(naphthalen-1-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one - 158938 3.1.3.48 (2E)-3-(naphthalen-1-yl)-1-(3-nitrophenyl)prop-2-en-1-one 12% inhibition at 0.025 mM 158940 3.1.3.48 (2E)-3-(naphthalen-1-yl)-1-(4-nitrophenyl)prop-2-en-1-one 18% inhibition at 0.025 mM 158919 3.1.3.48 (2E)-3-(naphthalen-1-yl)-1-phenylprop-2-en-1-one 37% inhibition at 0.025 mM 158805 3.1.3.48 (2E)-3-(naphthalen-2-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one 9% activation at 0.025 mM 158939 3.1.3.48 (2E)-3-(naphthalen-2-yl)-1-(3-nitrophenyl)prop-2-en-1-one 16% inhibition at 0.025 mM 158837 3.1.3.48 (2E)-3-(naphthalen-2-yl)-1-(4-nitrophenyl)prop-2-en-1-one 11% inhibition at 0.025 mM 158893 3.1.3.48 (2E)-3-(naphthalen-2-yl)-1-phenylprop-2-en-1-one 12% inhibition at 0.025 mM 158962 3.1.3.48 (2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one a semisynthetic licochalcone A derivative 79191 3.1.3.48 (2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one a semisynthetic licochalcone A derivative 79194 3.1.3.48 (2E)-3-[4-hydroxy-2-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 79195 3.1.3.48 (2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 14983 3.1.3.48 (2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one a semisynthetic licochalcone A derivative 79193 3.1.3.48 (2E)-3-[4-hydroxy-2-methoxy-5-(3-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 79198 3.1.3.48 (2E)-3-[5-bromo-2-hydroxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one - 85250 3.1.3.48 (2E)-3-[5-bromo-2-methoxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one - 85249 3.1.3.48 (2R)-2-benzyl-3-[2,6-dibromo-4-(6-bromo-5a,11a-dihydrobenzo[b]naphtho[2,3-d]furan-11-yl)phenyl]propanoic acid - 63575 3.1.3.48 (2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one - 230640 3.1.3.48 (2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one - 230642 3.1.3.48 (3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid - 230643 3.1.3.48 (3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate no inhibition at 0.020 mM 230644 3.1.3.48 (3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate no inhibition at 0.025 mM 230645 3.1.3.48 (3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate no inhibition at 0.024 mM 230646 3.1.3.48 (3beta)-3-(acetyloxy)olean-12-en-28-oic acid - 197192 3.1.3.48 (3beta)-3-hydroxyolean-12-en-28-oic acid - 188372 3.1.3.48 (3beta)-3-hydroxyoleana-11,13(18)-dien-28-oic acid - 197191 3.1.3.48 (3S,3aR,4S,5R,7aR)-4-acetyl-7-henicosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,5,7a-hexahydro-2-benzofuran-5-carboxylic acid - 197185 3.1.3.48 (3S,3aR,4S,7R,7aS)-4-acetyl-7-icosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,7,7a-hexahydro-2-benzofuran-5-carboxylic acid - 197184 3.1.3.48 (3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione - 85208 3.1.3.48 (3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone - 85210 3.1.3.48 (3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione - 85209 3.1.3.48 (3Z)-5-bromo-3-[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one - 197227 3.1.3.48 (4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate 50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F 129714 3.1.3.48 (4-fluorophenyl)[[(Z)-(2,2,2-trifluoro-1-[1-(4-fluorophenyl)-2-methyl-5-[4-(methylsulfonyl)phenyl]-1H-pyrrol-3-yl]ethylidene)amino]oxy]methanone - 197232 3.1.3.48 (4-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-methoxy-3-oxopropyl]phenyl)methaneseleninic acid inactivates the PTPs, e.g. YopH, by covalent modification, binds at the active site Cys403, kinetics, overview 158856 3.1.3.48 (4aR,6aR,6bS,8aR,12aS,14aR,14bR)-8a-hydroxy-4,4,6a,6b,11,11,14b-heptamethyl-1,4a,5,6,6a,6b,7,8a,9,10,11,12,12a,14,14a,14b-hexadecahydropicene-3,8(2H,4H)-dione - 197190 3.1.3.48 (4aR,6aS,6bR,8aR,10S,12aR,12bR,14bS)-4a,10-dihydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicen-5(1H)-one - 197193 3.1.3.48 (4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40290 3.1.3.48 (4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40221 3.1.3.48 (4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid - 40246 3.1.3.48 (4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40249 3.1.3.48 (4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid - 40260 3.1.3.48 (4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40247 3.1.3.48 (4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40248 3.1.3.48 (4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid - 40251 3.1.3.48 (4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid - 40225 3.1.3.48 (4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid - 40250 3.1.3.48 (4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid - 27282 3.1.3.48 (4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid no inhibition of LMW-PTP isozymes, but 20% inhibition of PTP-B1 at 0.02 mM 27282 3.1.3.48 (4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid - 40223 3.1.3.48 (4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-11-(methylamino)-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid - 79074 3.1.3.48 (4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid - 40233 3.1.3.48 (4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid - 40245 3.1.3.48 (4E)-2-(3,4-dichlorophenyl)-4-(3,4,5-trimethoxybenzylidene)-1,3-oxazol-5(4H)-one - 197234 3.1.3.48 (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid - 197244 3.1.3.48 (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazol-1-yl]pentanoic acid - 197255 3.1.3.48 (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,6a,9a,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d][1,2]oxazol-1-yl]pentanoic acid - 197246 3.1.3.48 (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid competitive PTP1B inhibitor 197245 3.1.3.48 (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoic acid - 197254 3.1.3.48 (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid - 197247 3.1.3.48 (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoic acid - 197252 3.1.3.48 (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,8,11a,13a-pentamethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid - 197248 3.1.3.48 (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid - 197250 3.1.3.48 (5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid - 230686 3.1.3.48 (5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13840 3.1.3.48 (5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13839 3.1.3.48 (5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione - 197165 3.1.3.48 (5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione - 197172 3.1.3.48 (5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione - 197178 3.1.3.48 (5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione - 197171 3.1.3.48 (5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione - 197177 3.1.3.48 (5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione - 197146 3.1.3.48 (5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione - 197148 3.1.3.48 (5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197155 3.1.3.48 (5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione - 197161 3.1.3.48 (5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione - 197153 3.1.3.48 (5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione - 197151 3.1.3.48 (5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197158 3.1.3.48 (5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione - 197164 3.1.3.48 (5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione - 197147 3.1.3.48 (5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione - 197166 3.1.3.48 (5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione - 197170 3.1.3.48 (5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione - 197169 3.1.3.48 (5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione - 197168 3.1.3.48 (5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione - 197167 3.1.3.48 (5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione - 197152 3.1.3.48 (5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197160 3.1.3.48 (5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione - 197154 3.1.3.48 (5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione - 197179 3.1.3.48 (5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione - 197176 3.1.3.48 (5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione - 197175 3.1.3.48 (5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione - 197174 3.1.3.48 (5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione - 197173 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione - 197149 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197156 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione - 197162 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197157 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione - 197163 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione - 197150 3.1.3.48 (5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione - 197159 3.1.3.48 (6aS,6bR,8aR,10S,12aS,12bR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b-hexadecahydropicen-5(1H)-one - 197194 3.1.3.48 (6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione - 85204 3.1.3.48 (7bS,9R,13bR,15R)-7-amino-9-(hydroxymethyl)-10,13-dioxo-2,3,3a,3b,4,5,6,7,7a,7b,9,10,13,13b-tetradecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-15-carbonitrile inhibits Cdc25B modestly 138667 3.1.3.48 (7bS,9R,13bR,15S)-7-amino-15-hydroxy-9-(hydroxymethyl)-2,3,3a,3b,4,5,6,7,7a,7b,9,13b-dodecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-10,13-dione - 138668 3.1.3.48 (9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione - 85207 3.1.3.48 (9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione - 85206 3.1.3.48 (difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid 50% inhibition at 163 nM for PTP-1B wild-type, at 1903 nM for PTP-1B mutant L119V, and at 1600 nM for isoform TCPTP wild-type and 138 nM for TCPTP mutant V121L 129700 3.1.3.48 (difluoro[4-[(2,2,2-trifluoroethyl)carbamoyl]phenyl]methyl)phosphonic acid - 79128 3.1.3.48 (difluoro[4-[(2-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid - 79129 3.1.3.48 (difluoro[4-[(2-phenylethyl)carbamoyl]phenyl]methyl)phosphonic acid - 79224 3.1.3.48 (difluoro[4-[(3-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid - 79127 3.1.3.48 (difluoro[4-[(4-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid - 79132 3.1.3.48 (difluoro[4-[(phenylamino)methyl]phenyl]methyl)phosphonic acid - 79133 3.1.3.48 (difluoro[4-[2-oxo-2-(phenylamino)ethyl]phenyl]methyl)phosphonic acid - 78897 3.1.3.48 (difluoro[4-[methyl(phenyl)carbamoyl]phenyl]methyl)phosphonic acid - 79131 3.1.3.48 (E)-N-(4,5-diphenyl-1,3-thiazol-2-yl)-2-naphthalen-2-ylethenesulfonamide - 63571 3.1.3.48 (E)-N-[4-(4-chlorophenyl)-5-propyl-1,3-thiazol-2-yl]-2-(3,4-dichlorophenyl)ethenesulfonamide - 63572 3.1.3.48 (Z)-1-(3-(3-carboxy-3-hydroxyacryloyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 2.4 mg/ml 197221 3.1.3.48 (Z)-1-(3-(4-ethoxy-3-hydroxy-4-oxobut-2-enoyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 3.1 mg/ml 197220 3.1.3.48 (Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25907 3.1.3.48 (Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid - 25893 3.1.3.48 (Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid NSC-117199 25892 3.1.3.48 (Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid - 25894 3.1.3.48 (Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid - 25895 3.1.3.48 (Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25911 3.1.3.48 (Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25906 3.1.3.48 (Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25910 3.1.3.48 (Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25902 3.1.3.48 (Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25913 3.1.3.48 (Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25903 3.1.3.48 (Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25908 3.1.3.48 (Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25900 3.1.3.48 (Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25905 3.1.3.48 (Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25912 3.1.3.48 (Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25904 3.1.3.48 (Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid - 25909 3.1.3.48 (Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid - 25901 3.1.3.48 ([2-bromo-4-(3-oxo-2,3-diphenylpropyl)phenyl](difluoro)methyl)phosphonic acid - 138186 3.1.3.48 1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione) - 197197 3.1.3.48 1,2-Cyclohexanedione 40% inhibition at 1 mM 2324 3.1.3.48 1,3-difluoro-2-[(E)-2-nitroethenyl]benzene 50% inhibition at 0.0048 mM in absence of 2-mercaptoethanol, at 0.34 mM in presence of 1 mM 2-mercaptoethanol 129696 3.1.3.48 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 15.1% inhibition at 0.02 mg/ml 197207 3.1.3.48 1,6-dimethyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione - 197238 3.1.3.48 1-(1,3-benzodioxol-5-yl)-2-([1-(4-hydroxyphenyl)-1H-1,2,3,4-tetraazol-5-yl]sulfanyl)-1-ethanone 88% inhibition at 0.2 mM 230736 3.1.3.48 1-(2,6-dihydroxy-4-methoxy-3-methylphenyl)ethanone isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 79285 3.1.3.48 1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 36.2% inhibition at 0.02 mg/ml 197202 3.1.3.48 1-(4-hydroxy-3-(methoxycarbonyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 8.1 mg/ml 197218 3.1.3.48 1-benzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 15.1% inhibition at 0.02 mg/ml 197200 3.1.3.48 1-benzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3.1% inhibition at 0.02 mg/ml 197201 3.1.3.48 1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 0.7% inhibition at 0.02 mg/ml 197204 3.1.3.48 1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 0.8% inhibition at 0.02 mg/ml 197198 3.1.3.48 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3.5% inhibition at 0.02 mg/ml 197199 3.1.3.48 1-cyclopropyl-N-(4-fluorobenzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 3.3% inhibition at 0.02 mg/ml 197212 3.1.3.48 1-ethyl-3-dimethylaminopropyl carbodiimide 90% inhibition at 25 mM 109998 3.1.3.48 1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione covalent mode of action 58175 3.1.3.48 1-methoxy-4-((E)-2-nitrovinyl)benzene 50% inhibition at 0.0045 mM in absence of 2-mercaptoethanol, at 0.27 mM in presence of 1 mM 2-mercaptoethanol 129278 3.1.3.48 1-methyl-4-((E)-2-nitrovinyl)benzene 50% inhibition at 0.003 mM in absence of 2-mercaptoethanol, at 0.225 mM in presence of 1 mM 2-mercaptoethanol 129279 3.1.3.48 1-p-Bromotetramisole oxalate tetramizole no effect 90589 3.1.3.48 1-[(5Z)-5-(1-butyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperidine-4-carboxamide - 197228 3.1.3.48 1-[4-[(2-nitrophenyl)sulfonyl]piperazin-1-yl]-2-phenoxyethanone - 197226 3.1.3.48 15-hydroxykaur-9(11),16-dien-19-oic acid - 230886 3.1.3.48 16alphaH,17-isovaleryloxy-ent-kauran-19-oic acid diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.007 mM, noncompetitive 58174 3.1.3.48 19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid - 71560 3.1.3.48 2',4'-dihydroxy-1,1'-biphenyl - 78989 3.1.3.48 2,2'-[benzene-1,4-diylbis(methanediyloxybenzene-4,1-diyl)]bis(oxoacetic acid) - 197257 3.1.3.48 2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide competitive, noncovalent mode of action 58176 3.1.3.48 2,4-dihydroxy-6-methylbenzoic acid 45% inhibition of PTPB1 at 0.178 mM 159652 3.1.3.48 2,4-dimethoxy-1-((E)-2-nitrovinyl)benzene 50% inhibition at 0.028 mM in absence of 2-mercaptoethanol, at 0.390 mM in presence of 1 mM 2-mercaptoethanol 129282 3.1.3.48 2,5-dihydroxy-3-[7-(2-methylbenzyl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione - 63569 3.1.3.48 2,5-dihydroxy-3-[7-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione - 63570 3.1.3.48 2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid i.e. OATP 13835 3.1.3.48 2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13838 3.1.3.48 2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13837 3.1.3.48 2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13836 3.1.3.48 2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid - 13866 3.1.3.48 2-(2,5-dimethyl-1H-pyrrol-1-yl)-5-hydroxybenzoic acid 36% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 7% residual activity at 0.1 mM; 9% residual activity at 0.1 mM 24978 3.1.3.48 2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27291 3.1.3.48 2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27266 3.1.3.48 2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid - 117278 3.1.3.48 2-(oxalyl-amino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid - 117277 3.1.3.48 2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid - 17246 3.1.3.48 2-carboperoxybenzoate complete inhibition at 150 mM 146535 3.1.3.48 2-chloro-4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 36% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 95% residual activity at 0.1 mM; 98% residual activity at 0.1 mM 24982 3.1.3.48 2-chloro-5-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 37% residual activity at 0.1 mM; 77% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 91% residual activity at 0.1 mM 24984 3.1.3.48 2-hydroperoxytetrahydrofuran inactivation by 2-hydroperoxytetrahydrofuran (0.05 mM, 10 min) is reversed upon reaction of the enzyme with dithiothreitol (54% return of activity, following treatment with 100 mM dthiothreitol for 1 h) 147223 3.1.3.48 2-mercaptoethanol - 63 3.1.3.48 2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino]-1H-indene-1,3(2H)-dione - 188253 3.1.3.48 2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid i.e. TCS401, binds to the active site 232720 3.1.3.48 2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-6-hydroxy-3-oxo-3H-xanthen-9-yl]benzoic acid i.e. FlAsH 231092 3.1.3.48 2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide mixed-type inhibition, 99% inhibition at 0.2 mM 231101 3.1.3.48 24-hydroxyursolic acid - 38299 3.1.3.48 28-(10-decanoic)-oleanolic acid - 70667 3.1.3.48 28-(12-dodecanoic)-oleanolic acid - 70668 3.1.3.48 28-(2-acetic)-oleanolic acid - 70669 3.1.3.48 28-(4-butyric)-oleanolic acid - 70670 3.1.3.48 28-(6-hexanoic)-oleanolic acid - 70671 3.1.3.48 28-(8-octanoic)-oleanolic acid - 70672 3.1.3.48 28-(glycine)-oleanolic acid amide - 70673 3.1.3.48 28-(L-glutamic acid)-oleanolic acid amide - 70674 3.1.3.48 28-(L-phenylalanine)-oleanolic acid amide - 70675 3.1.3.48 28-(p-carboxyphenyl)-oleanolic acid amide - 70676 3.1.3.48 28-[4-butyric((R)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene - 70677 3.1.3.48 28-[4-butyric((S)-1-carboxy-3-indole-ethyl)-amide]-DELTA12-oleanene - 70678 3.1.3.48 28-[4-butyric((S)-1-carboxy-5-imidazole-ethyl)-amide]-DELTA12-oleanene - 70679 3.1.3.48 28-[4-butyric((S)-1-carboxy-methylthioethyl)-amide]-DELTA12-oleanene - 70680 3.1.3.48 28-[4-butyric((S)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene - 70681 3.1.3.48 28-[4-butyric(1-carboxy-2,3-dimethoxyphenylethyl)-amide]-DELTA12-oleanene - 70682 3.1.3.48 28-[4-butyric(1-carboxy-3,4-dimethoxyphenylethyl)-amide]-DELTA12-oleanene - 70683 3.1.3.48 28-[4-butyric(1-carboxy-3,4-oxymethyleneoxyphenylethyl)-amide]-DELTA12-oleanene - 70684 3.1.3.48 28-[4-butyric(1-carboxy-3,5-dimethoxyphenylethyl)-amide]-DELTA12-oleanene - 70685 3.1.3.48 28-[4-butyric(1-carboxy-m-chlorophenylethyl)-amide]-DELTA12-oleanene - 70686 3.1.3.48 28-[4-butyric(1-carboxy-m-methoxyphenylethyl)-amide]-DELTA12-oleanene - 70687 3.1.3.48 28-[4-butyric(1-carboxy-o-chlorophenylethyl)-amide]-DELTA12-oleanene - 70688 3.1.3.48 28-[4-butyric(1-carboxy-o-methoxyphenylethyl)-amide]-DELTA12-oleanene - 70689 3.1.3.48 28-[4-butyric(1-carboxy-o-methylphenylethyl)-amide]-DELTA12-oleanene - 70690 3.1.3.48 28-[4-butyric(1-carboxy-p-chlorophenylethyl)-amide]-DELTA12-oleanene - 70691 3.1.3.48 28-[4-butyric(1-carboxy-p-fluorophenylethyl)-amide]-DELTA12-oleanene - 70692 3.1.3.48 28-[4-butyric(1-carboxy-p-methoxyphenylethyl)-amide]-DELTA12-oleanene - 70693 3.1.3.48 28-[4-butyric(1-carboxy-p-methylphenylethyl)-amide]-DELTA12-oleanene - 70694 3.1.3.48 28-[4-butyric(1-carboxy-p-nitrophenylethyl)-amide]-DELTA12-oleanene - 70695 3.1.3.48 2alpha,3alpha,19alpha,23-tetrahydroxyurs-12-en-28-oic acid 50% inhibition at 0.0421 mM 129284 3.1.3.48 2beta,3beta-2,3-dihydroxyolean-12-en-28-oic acid - 79257 3.1.3.48 3',4'-dihydroxy-1,1'-biphenyl no inhibition of LMW-PTP isozymes, but 5% inhibition of PTP-B1 at 0.02 mM 158878 3.1.3.48 3,16-dioxo-olean-12(13),17(18)-diene - 197188 3.1.3.48 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop 129707 3.1.3.48 3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop 129706 3.1.3.48 3-(1-carboxy-ethoxy)-6-chloro-benzo(b)-thiophene-2-carboxylic acid - 58185 3.1.3.48 3-(2,2'-dimethyl-carboxypropanoyloxy)-oleanolic acid - 70699 3.1.3.48 3-(2,5-dimethyl-1H-pyrrol-1-yl)-4-hydroxybenzoic acid 20% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 52% residual activity at 0.1 mM; 7% residual activity at 0.1 mM 24979 3.1.3.48 3-(2-carboxy-benzyloxy)-oleanolic acid - 70718 3.1.3.48 3-(2-carboxybenzoyloxy)-oleanolic acid - 70717 3.1.3.48 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide 50% inhibition of PTP1B at 0.35 mM 129285 3.1.3.48 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide - 197195 3.1.3.48 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-yl-sulfamyl)-phenyl)-amide a PTP1b inhibitor, inhibit 50% tog the infectivity of Trypanosoma cruzi trypomastigotes 165929 3.1.3.48 3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide i.e. BBR 232721 3.1.3.48 3-(3-carboxy-benzyloxy)-oleanolic acid - 70719 3.1.3.48 3-(4-carboxy-benzyloxy)-28-[4-butyric((s)-1-carboxyphenylethyl)-amide]-DELTA12-oleanene - 71555 3.1.3.48 3-(4-carboxy-benzyloxy)-oleanolic acid - 70720 3.1.3.48 3-(4-chlorophenyl)-1,6-dimethylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione - 197239 3.1.3.48 3-(biphenyl-4-ylmethyl)-6-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one - 159650 3.1.3.48 3-(carboxy-fluoro-methoxy)-6-chloro-benzo(b)thiophene-2-carboxylic acid - 58186 3.1.3.48 3-(carboxymethoxy)-2-naphthoic acid - 58178 3.1.3.48 3-(carboxymethoxy)-5-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58199 3.1.3.48 3-(carboxymethoxy)-5-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58201 3.1.3.48 3-(carboxymethoxy)-5-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58197 3.1.3.48 3-(carboxymethoxy)-6-((1-(ethylsulfonyl)-piperidin-4-yl)amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 129708 3.1.3.48 3-(carboxymethoxy)-6-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58200 3.1.3.48 3-(carboxymethoxy)-6-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58202 3.1.3.48 3-(carboxymethoxy)-6-(tetrahydro-2H-pyran-4-ylamino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58203 3.1.3.48 3-(carboxymethoxy)-6-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58198 3.1.3.48 3-(carboxymethoxy)-6-methylthieno(3,2-c)pyridine-2-carboxylic acid - 58181 3.1.3.48 3-(carboxymethoxy)benzo(b)thiophene-2-carboxylic acid - 58180 3.1.3.48 3-(carboxymethoxy)furo(2,3-b)pyridine-2-carboxylic acid - 58179 3.1.3.48 3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid reversible, competitive 35363 3.1.3.48 3-(carboxymethoxy)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid - 58196 3.1.3.48 3-(carboxymethoxy)thieno(3,2-b)pyridine-2-carboxylic acid - 58182 3.1.3.48 3-(carboxymethoxy)thieno(3,2-b)thiophene-2-carboxylic acid - 58183 3.1.3.48 3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid - 231229 3.1.3.48 3-benzyl-7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM 158947 3.1.3.48 3-benzyloxy-oleanolic acid - 70735 3.1.3.48 3-butyl-7-(2,4-dihydroxy-6-pentylphenoxy)-3,5-dimethoxy-2-benzofuran-1(3H)-one a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78871 3.1.3.48 3-carboxymethoxy-6-(4-hydroxyphenyl)-benzo(b)-thiophene-2-carboxylic acid - 58189 3.1.3.48 3-carboxymethoxy-6-(5-methyl-1-phenyl-1H-pyrazol-3-ylcarbamoyl)-benzo(b)thiophene-2-carboxylic acid - 58191 3.1.3.48 3-carboxymethoxy-6-chloro-benzo(b)-thiophene-2-carboxylic acid - 58184 3.1.3.48 3-carboxymethoxy-6-phenylbenzo(b)-thiophene-2-carboxylic acid - 58188 3.1.3.48 3-carboxymethoxy-6-thiophen-2-yl-benzo(b)-thiophene-2-carboxylic acid - 58190 3.1.3.48 3-carboxymethoxy-7-chloro-benzo(b)-thiophene-2-carboxylic acid - 58192 3.1.3.48 3-carboxymethoxy-7-methyl-benzo(b)-thiophene-2-carboxylic acid - 58193 3.1.3.48 3-carboxymethoxy-naphtho(1,2-b)thiophene-2-carboxylic acid - 58194 3.1.3.48 3-carboxymethoxy-thieno(3,2-c)quinoline-2-carboxylic acid - 58195 3.1.3.48 3-carboxypropanoyloxy-oleanolic acid - 70741 3.1.3.48 3-chlorobenzenecarboperoxoic acid complete inhibition at 150 mM 146545 3.1.3.48 3-dehydroxy-oleanolic acid - 70742 3.1.3.48 3-ethyl oxalyl-oleanolic acid - 70743 3.1.3.48 3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl 3-acetyl-2,4-dihydroxy-6-methylbenzoate isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78858 3.1.3.48 3-hydroxy-4-(methoxycarbonyl)-5-methylphenyl 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoate - 79095 3.1.3.48 3-methyl-2-butenal 95% remaining activity at 0.5 mM 7441 3.1.3.48 3-methylene-oleanolic acid - 70744 3.1.3.48 3-oxalyl-oleanolic acid - 70745 3.1.3.48 3-oxo-oleanolic acid - 70746 3.1.3.48 3-[(1-butyl-1,6-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-4-yl)oxy]-4,6-dihydroxy-2-pentylbenzoic acid a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 79159 3.1.3.48 3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide - 25898 3.1.3.48 3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide - 25899 3.1.3.48 3-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158780 3.1.3.48 3-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158778 3.1.3.48 3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid - 231330 3.1.3.48 3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid irreversible inhibition, detailed kinetic analysis of the interaction between E4 and the catalytic domain of enzyme STEP, overview. kinact is 0.068/s 231336 3.1.3.48 3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one - 231338 3.1.3.48 3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid - 25896 3.1.3.48 3-[oxalyl-amino]naphthalene-2-carboxylic acid - 117276 3.1.3.48 3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,6-dicarboxylic acid 25% residual activity at 0.1 mM; 39% residual activity at 0.1 mM; 65% residual activity at 0.1 mM; 73% residual activity at 0.1 mM 24977 3.1.3.48 3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid 30% residual activity at 0.1 mM; 53% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 79% residual activity at 0.1 mM 24974 3.1.3.48 3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 23% residual activity at 0.1 mM; 75% residual activity at 0.1 mM; 80% residual activity at 0.1 mM; 9% residual activity at 0.1 mM 24972 3.1.3.48 3alpha-angeloyloxypterokaurene L3 18% inhibition at 0.024 mM 231358 3.1.3.48 3alpha-cinnamoyloxypterokaurene L3 - 231359 3.1.3.48 3alpha-oleanolic acid - 70734 3.1.3.48 3alpha-tigloyloxypterokaurene L3 no inhibition at 0.024 mM 231360 3.1.3.48 3beta,16a,17-trihydroxy-olean-12-ene - 197189 3.1.3.48 3beta-acetoxy-17beta-hydroxy-28-norolean-12-ene - 71566 3.1.3.48 3beta-acetoxy-28-hydroxyolean-12-ene - 71563 3.1.3.48 3beta-acetoxyolean-12-en-28-acid - 71564 3.1.3.48 3beta-acetoxyolean-12-en-28-aldehyde - 71565 3.1.3.48 3beta-hydroxyolean-12-en-28-oic acid - 35107 3.1.3.48 4'-carboxy-3'-hydroxy-1,1'-biphenyl no inhibition of LMW-PTP isozymes, but 10% inhibition of PTP-B1 at 0.02 mM 158800 3.1.3.48 4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol - 78962 3.1.3.48 4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol - 78916 3.1.3.48 4,4'-[benzene-1,4-diylbis(methanediyloxy)]dibenzoic acid - 70752 3.1.3.48 4,6-bis(1,3,2-dithiarsolan-2-yl)-7-hydroxy-3H-phenoxazin-3-one i.e. ReAsH 231374 3.1.3.48 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid - 231384 3.1.3.48 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid - 231385 3.1.3.48 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid - 231386 3.1.3.48 4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid - 231387 3.1.3.48 4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid - 231388 3.1.3.48 4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid - 231389 3.1.3.48 4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid - 231390 3.1.3.48 4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid - 231391 3.1.3.48 4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid 50% inhibition at 39 nM for wild-type PTP-1B, at 39 nM for mutant V113I, at 45 nM for mutant M114V, at 29 nM for mutant V113I/M114V, at 32 nM for mutant G117E, at 142 nM for mutant L119V, and at 87 nM for isoform TCPTP wild-type and 24 nM for isoform TCPTP mutant V121L 129698 3.1.3.48 4-((E)-2-nitrovinyl)benzoic acid 50% inhibition at 0.0027 mM in absence of 2-mercaptoethanol, at 0.425 mM in presence of 1 mM 2-mercaptoethanol 129280 3.1.3.48 4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 63% residual activity at 0.1 mM; 6% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 9% residual activity at 0.1 mM 24981 3.1.3.48 4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoic acid 21% residual activity at 0.1 mM; 67% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 9% residual activity at 0.1 mM 24980 3.1.3.48 4-(2,5-dimethyl-1H-pyrrol-1-yl)phthalic acid 18% residual activity at 0.1 mM; 54% residual activity at 0.1 mM; 78% residual activity at 0.1 mM; 80% residual activity at 0.1 mM 24985 3.1.3.48 4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid - 197196 3.1.3.48 4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid - 231420 3.1.3.48 4-(5-[5-(3,5-dichlorophenoxy)-2-furyl]-1,2,4-oxadiazol-3-yl)phenyl-N,N-dimethylsulfamate 85% inhibition at 0.2 mM 231421 3.1.3.48 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoic acid - 79245 3.1.3.48 4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide - 59327 3.1.3.48 4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide dose-dependent increase in Y527 phosphorylation of Src 129704 3.1.3.48 4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231428 3.1.3.48 4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231429 3.1.3.48 4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231430 3.1.3.48 4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231431 3.1.3.48 4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231432 3.1.3.48 4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231433 3.1.3.48 4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231434 3.1.3.48 4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231435 3.1.3.48 4-([(5E)-5-[3-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 156867 3.1.3.48 4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231436 3.1.3.48 4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid - 231437 3.1.3.48 4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid - 231438 3.1.3.48 4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid - 231439 3.1.3.48 4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid - 231440 3.1.3.48 4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid - 231441 3.1.3.48 4-([(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid - 158763 3.1.3.48 4-chloro-N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide - 158770 3.1.3.48 4-chloro-N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide - 158769 3.1.3.48 4-chloro-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide - 159006 3.1.3.48 4-chloro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide - 158767 3.1.3.48 4-fluoro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide - 158766 3.1.3.48 4-fluorobenzyl-1-cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate 73% inhibition at 0.02 mg/ml 197210 3.1.3.48 4-hydroxymercuribenzoate 62% inhibition at 2.5 mM 970 3.1.3.48 4-isoavenaciolide potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR 36978 3.1.3.48 4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-(4-methoxyphenyl)isoxazole - 63578 3.1.3.48 4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-phenylisoxazole - 63577 3.1.3.48 4-methoxy-N-(6-methoxy-1,3-benzothiazol -2-yl)benzenesulfonamide - 158764 3.1.3.48 4-methoxy-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide - 158983 3.1.3.48 4-methoxy-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide - 158840 3.1.3.48 4-methyl-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide - 158758 3.1.3.48 4-methyl-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide - 158762 3.1.3.48 4-nitro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide - 158988 3.1.3.48 4-nitrocatechol sulfate applied from from bare and amine functionalized mesoporous silica, MCM-48, and mesoporous alumina for sustained delivery, competitive inhibition, kinetics, overview 2884 3.1.3.48 4-nitrophenyl phosphate substrate inhibition at higher concentrations; substrate inhibition at higher concentrations 136 3.1.3.48 4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129252 3.1.3.48 4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM 129271 3.1.3.48 4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde 50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129264 3.1.3.48 4-oxo-6-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129270 3.1.3.48 4-oxo-8-(phenylsulfanyl)-1,4-dihydro-1,7-naphthyridine-3-carboxylic acid - 63573 3.1.3.48 4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129269 3.1.3.48 4-[(1E)-3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-5-methoxy-2-(2-methylbut-3-en-2-yl)phenyl acetate a semisynthetic licochalcone A derivative 79300 3.1.3.48 4-[(2,4-dihydroxy-6-pentadecylbenzoyl)oxy]-2-hydroxy-6-methylbenzoic acid - 78875 3.1.3.48 4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-bromobenzoate - 85221 3.1.3.48 4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-tert-butylbenzoate - 85222 3.1.3.48 4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl benzoate - 85220 3.1.3.48 4-[(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate a semisynthetic licochalcone A derivative 79274 3.1.3.48 4-[(2E)-3-[4-(acetyloxy)-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate a semisynthetic licochalcone A derivative 78889 3.1.3.48 4-[(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate a semisynthetic licochalcone A derivative 78888 3.1.3.48 4-[(3-[(E)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158804 3.1.3.48 4-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158824 3.1.3.48 4-[(4-[(Z)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158935 3.1.3.48 4-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid - 158803 3.1.3.48 4-[1,3-dioxo-5-(4-oxo-4H-3,1-benzoxazin-2-yl)-1,3-dihydro-2H-isoindol-2-yl]benzoate - 197230 3.1.3.48 4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid - 231485 3.1.3.48 4-[4,5-di(biphenyl-4-yl)-1H-imidazol-2-yl]benzoic acid - 197231 3.1.3.48 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoic acid - 85219 3.1.3.48 4-[difluoro(phosphono)methyl]benzoic acid - 78979 3.1.3.48 4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid - 25897 3.1.3.48 4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231487 3.1.3.48 4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231488 3.1.3.48 4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231489 3.1.3.48 4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231490 3.1.3.48 4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231491 3.1.3.48 4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231492 3.1.3.48 4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231493 3.1.3.48 4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231494 3.1.3.48 4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231495 3.1.3.48 4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231496 3.1.3.48 4-[[(2Z,5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158808 3.1.3.48 4-[[(2Z,5E)-5-[3-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158807 3.1.3.48 4-[[(2Z,5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158791 3.1.3.48 4-[[(2Z,5Z)-5-[4-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158799 3.1.3.48 4-[[(5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158797 3.1.3.48 4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231497 3.1.3.48 4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231498 3.1.3.48 4-[[(5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid - 158958 3.1.3.48 4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231499 3.1.3.48 4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid - 231500 3.1.3.48 5,7-bis[(E)-2-[4-(dimethylamino)phenyl]ethenyl]-2-methyltetrazolo[1,5-a]pyrimidin-2-ium - 197233 3.1.3.48 5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E)-3-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]prop-1-en-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium i.e. AsCy3, 70% inhibition at 250 nM AsCy3, AsCy3 is capable of specifically and potently inhibiting mutant enzyme asPTP1B in the presence of a complex proteome, while AsCy3 does not inhibit wild-type PTP1B activity in a cell lysate 231514 3.1.3.48 5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E,5E)-5-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]penta-1,3-dien-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium i.e. AsCy5 231515 3.1.3.48 5-(2-fluoro-5-((1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]prop-1-en-1-yl)phenyl)isoxazole-3-carboxylic acid - 138188 3.1.3.48 5-([(E)-[2-(4-chlorophenyl)-5-oxo-1,3-oxazol-4(5H)-ylidene]methyl]amino)-2-hydroxybenzoic acid - 197237 3.1.3.48 5-([1-[(2-chloro-1,3-thiazol-5-yl)methyl]-1H-indol-3-yl]methylidene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione - 197240 3.1.3.48 5-acetylamino-2-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid 45% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 82% residual activity at 0.1 mM; 94% residual activity at 0.1 mM 24983 3.1.3.48 5-chloro-2-[methyl(methylidene)-lambda4-sulfanyl]-6-[(naphthalen-2-yl)oxy]-1H-benzimidazole 65% inhibition at 0.2 mM 231526 3.1.3.48 5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide mixed-type inhibition, complete inhibition at 0.2 mM 231533 3.1.3.48 5-methoxy-4-[(1E)-3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-2-(2-methylbut-3-en-2-yl)phenyl acetate a semisynthetic licochalcone A derivative 79010 3.1.3.48 5-[3-bromo-4-[(4-nitrobenzyl)oxy]benzylidene]pyrimidine-2,4,6(1H,3H,5H)-trione - 197229 3.1.3.48 5-[4-(3,4-dihydroisoquinolin-2(1H)-yl)-3-nitrobenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 197236 3.1.3.48 5-[4-[(2-chloro-6-fluorobenzyl)oxy]benzylidene]-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione - 197241 3.1.3.48 6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27280 3.1.3.48 6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129276 3.1.3.48 6-((1-(benzylsulfonyl)piperidin-4-yl)amino)-3-(carboxymethoxy)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid - 58204 3.1.3.48 6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM 129268 3.1.3.48 6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129257 3.1.3.48 6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129266 3.1.3.48 6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129260 3.1.3.48 6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129267 3.1.3.48 6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM 129254 3.1.3.48 6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM 129694 3.1.3.48 6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM 129695 3.1.3.48 6-(4-(3-(3-(benzyloxy)-2-(methoxycarbonyl)phenoxy)propyl)piperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of 45.2 mg/ml 197224 3.1.3.48 6-(4-benzylpiperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 62.3% inhibition at 0.02 mg/ml 197208 3.1.3.48 6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129255 3.1.3.48 6-amino-1-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 12.4% inhibition at 0.02 mg/ml 197203 3.1.3.48 6-benzyl-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 87.5% inhibition at 0.02 mg/ml 197205 3.1.3.48 6-benzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129274 3.1.3.48 6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129272 3.1.3.48 6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde 50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM 129273 3.1.3.48 6-bromo-3-carboxymethoxy-benzo(b)-thiophene-2-carboxylic acid - 58187 3.1.3.48 6-bromo-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129253 3.1.3.48 6-chloro-7-(2,3-dihydro-1H-inden-1-ylamino)quinoline-5,8-dione - 63565 3.1.3.48 6-chloro-7-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione - 63563 3.1.3.48 6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129262 3.1.3.48 6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129258 3.1.3.48 6-fluoro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 35% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 75% residual activity at 0.1 mM 24976 3.1.3.48 6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 20% inhibition of PTP-B1 at 0.015 mM 27293 3.1.3.48 6-hydroxy-2-phenyl-3-((3-trifluoromethyl)phenyl)benzofuran-5-carboxylic acid most potent, reversible and noncompetitive inhibitor, highly selective towards isoform PTPB 197180 3.1.3.48 6-hydroxy-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]-1H-1,2,3-triazol-4-yl]-2-phenyl-1-benzofuran-5-carboxylic acid - 63576 3.1.3.48 6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylate 80% residual activity at 0.1 mM 138788 3.1.3.48 6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 38% residual activity at 0.1 mM; 50% residual activity at 0.1 mM; 73% residual activity at 0.1 mM 36977 3.1.3.48 6-iodo-1-(4-methoxy-3-(methoxycarbonyl)benzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid IC50 of more than 20 mg/ml 197217 3.1.3.48 6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid - 231664 3.1.3.48 7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one - 231680 3.1.3.48 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2 231682 3.1.3.48 7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one - 231683 3.1.3.48 7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one - 231685 3.1.3.48 7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one - 231686 3.1.3.48 7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one - 231691 3.1.3.48 7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one - 231695 3.1.3.48 7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one - 231710 3.1.3.48 7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one - 231711 3.1.3.48 7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one - 231712 3.1.3.48 7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one - 231713 3.1.3.48 7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one - 231716 3.1.3.48 7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile 50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F 129283 3.1.3.48 7-chloro-6-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione - 63564 3.1.3.48 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 158845 3.1.3.48 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27279 3.1.3.48 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27272 3.1.3.48 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27273 3.1.3.48 7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one - 27271 3.1.3.48 7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM 158801 3.1.3.48 7-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one isolated from the CH2Cl2 extract of Glycyrrhiza inflata 78997 3.1.3.48 7-hydroxy-2-(4-hydroxyphenyl)-3-[(3',4'-dihydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one 60% inhibition of LMW-PTP isozyme 2, 25% inhibition of LMW-PTP 1, and 50% inhibition of PTP-B1, at 0.02 mM 158846 3.1.3.48 7-hydroxy-2-(4-hydroxyphenyl)-3-[(4'-carboxy-3'-hydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one 5% inhibition of LMW-PTP isozyme 2, 10% inhibition of LMW-PTP 1, and 59% inhibition of PTP-B1, at 0.02 mM 158847 3.1.3.48 7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 20% inhibition of PTP-B1 at 0.015 mM 27278 3.1.3.48 7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 10% inhibition of PTP-B1 at 0.015 mM 27275 3.1.3.48 7-hydroxy-2-(4-hydroxyphenylpropyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one 10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM 158760 3.1.3.48 8-acetyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 48% residual activity at 0.1 mM; 66% residual activity at 0.1 mM; 81% residual activity at 0.1 mM; 83% residual activity at 0.1 mM 24975 3.1.3.48 8-benzyl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129275 3.1.3.48 8-bromo-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid 33% residual activity at 0.1 mM; 41% residual activity at 0.1 mM; 8% residual activity at 0.1 mM; 90% residual activity at 0.1 mM 24973 3.1.3.48 8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde 50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129265 3.1.3.48 8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129256 3.1.3.48 8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129261 3.1.3.48 8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129263 3.1.3.48 8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde 50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases 129259 3.1.3.48 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylic acid isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78995 3.1.3.48 abietic acid a nonpolar inhibitor and weak mixed-type inhibitor of PTP1B, inhibits the enzyme by binding to its active site in a nonsubstrate-like manner that stabilizes the catalytically essential WPD loop in an inactive conformation, modelling of enzyme binding. Upon binding to the active site, abietic acid forms a hydrogen bond with R221 that weakens a bond between R221 and E115 and prevents the formation of a hydrogen bond between W179 and R221 that forms when the WPD loop closes 3524 3.1.3.48 acanthoic acid diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.024 mM 129251 3.1.3.48 acetaldehyde more than 95% remaining activity at 0.5 mM 90 3.1.3.48 Acetylsalicylic acid 80% inhibition at 0.2 mM 2261 3.1.3.48 acid - 31001 3.1.3.48 acrolein 4% remaining activity at 0.5 mM, potent irreversible time-dependent inhibitor, addition of 1 mM vanadate slows inactivation of PTP1B by 0.5 mM acrolein 1198 3.1.3.48 Ag+ 16.6% inhibition at 2 mM 75 3.1.3.48 Ag+ 62% inhibition at 2.5 mM 75 3.1.3.48 Ammonium molybdate complete inhibition of enzyme isolated from metacyclic stage, 75% inhibition of enzyme from procyclic stage 3327 3.1.3.48 Ammonium molybdate 4% residual activity in ovary and no activity in haemolymph at 1 mM 3327 3.1.3.48 Ammonium molybdate strong inhibition 3327 3.1.3.48 Ammonium molybdate 98% inhibition at 2 mM 3327 3.1.3.48 antimonate inhibition of protein tyrosine phosphatase activity 129693 3.1.3.48 aquastatin A derived from marine fungus Cosmospora sp. SF-5060, competitive inhibition 8854 3.1.3.48 arsenate inhibition of protein tyrosine phosphatase activity 255 3.1.3.48 ATP - 4 3.1.3.48 auranofin inhibition of cysteine-dependent protein tyrosine phosphatases 1894 3.1.3.48 benzenesulfonamide - 22586 3.1.3.48 benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate - 85205 3.1.3.48 benzyl 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylate 0.1% inhibition at 0.02 mg/ml 197216 3.1.3.48 benzyl 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate 80.5% inhibition at 0.02 mg/ml 197209 3.1.3.48 benzyl oleanolic acid amide - 70802 3.1.3.48 benzyl oleanolic acid ester - 70803 3.1.3.48 Berberine binding structure, molecular modeling, overview 1612 3.1.3.48 betulinic acid 95.1% PTP1B inhibitory activity with 0.0007 mg/ml 3725 3.1.3.48 betulinic acid methyl ester 89.4% PTP1B inhibitory activity with 0.00093 mg/ml 147227 3.1.3.48 biphenyl-3,4-diol 25% inhibition of LMW-PTP isozyme 2, and 10% inhibition of LMW-PTP 1 and PTP-B1 at 0.02 mM 14960 3.1.3.48 bis(2-ethyl-maltolato)oxidovanadium(IV) noncompetitive inhibition of hydrolysis of 4-nitrophenyl phosphate and of phosphorylated undecapeptide substrate EGFR988-998 in the presence of bis(2-ethyl-maltolato)oxidovanadium(IV) 232715 3.1.3.48 bis(2-methyl-maltolato)oxidovanadium(IV) - 232716 3.1.3.48 bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV) - 232717 3.1.3.48 bis(acetylacetonato)oxidovanadium(IV) acts as an uncompetitive inhibitor of PTP1B with DADEpYLIPQQG as the substrate, but this VO2+-chelate exhibits only apparent competitive inhibition of 4-nitrophenyl phosphate hydrolysis when catalyzed by PTP1B, differing from that observed in the hydrolysis of the phosphotyrosine-containing undecapeptide DADEpYLIPQQG mimicking residues 988-998 of the epidermal growth factor receptor (EGFR). Addition of 4-nitrophenyl phosphate after addition of saturating amounts of bis(acetylacetonato)oxidovanadium(IV) to PTP1B causes complete loss of catalytic activity 232714 3.1.3.48 BzN-EJJ-amide 50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F 58177 3.1.3.48 BzN-EJJ-amide 50% inhibition at 8nM for wild-type PTP-1B, at 14 nM for PTP-1B mutant V113I, at 7 nM for mutant M114V, at 7 nM for mutant V113I/M114V, at 11 nM for mutant G117E, at 12 nM for mutant L119V 58177 3.1.3.48 Ca2+ - 15 3.1.3.48 calopocarpin - 14890 3.1.3.48 cantharidin 17% inhibition at 1 mM 7414 3.1.3.48 chloro(1,3-dimethyl-1,3-dihydro-2H-imidazol-2-ylidene)gold i.e. [(p-MeMeIm)AuICl] 158873 3.1.3.48 chloro(1-methyl-1,3-dihydro-2H-imidazol-2-ylidene)gold i.e. [(MeIm)AuICl] 158874 3.1.3.48 chloro[1-methyl-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazol-2-yl]gold i.e. [(p-MeBzMeIm)AuICl] 158876 3.1.3.48 CinnGel 2ME 30.2% inhibition at 0.02 mM 38298 3.1.3.48 CinnGel 2ME the free cinnamic acid component of CinnGEL 2Me inhibits PTP1B 38298 3.1.3.48 Cl- - 141 3.1.3.48 continentalic acid modelling of enzyme binding 232718 3.1.3.48 corosolic acid 50% inhibition at 0.0072mM, mixed-type inhibition 17301 3.1.3.48 Cr(VI) as Na2CrO4, induces clonogenic lethality 159649 3.1.3.48 crotonaldehyde 85% remaining activity at 0.5 mM 1529 3.1.3.48 Cu2+ 32.2% inhibition at 2 mM 19 3.1.3.48 Cu2+ - 19 3.1.3.48 Cu2+ lung enzyme 19 3.1.3.48 cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 71.1% inhibition at 0.02 mg/ml 197206 3.1.3.48 dehydroabietic acid modelling of enzyme binding 183200 3.1.3.48 dehydrocostuslactone 86.2% PTP1B inhibitory activity with 0.00651 mg/ml 147229 3.1.3.48 dephostatin complete inhibition of enzyme isolated from metacyclic stage, 28% inhibition of enzyme from procyclic stage 12968 3.1.3.48 dephostatin - 12968 3.1.3.48 diethylcarbamazine 12% inhibition at 0.2 mM 51622 3.1.3.48 diethyldicarbonate 7% inhibition at 1 mM 310 3.1.3.48 Differentiation inducing factor 1 DIF-1, inhibits PTP3 by induction of serine-threonine phosphorylation of PTP3 159642 3.1.3.48 dihydroabietic acid modelling of enzyme binding 232719 3.1.3.48 diphosphate 1 mM, 31% residual activity 17 3.1.3.48 diphosphate - 17 3.1.3.48 disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate suramin-derivative, 50% inhibition at 0.030 mM, reversible and competitive 129702 3.1.3.48 disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate suramin-derivative, 50% inhibition of PTP1B at 0.010 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58898 3.1.3.48 disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate suramin-derivative, 50% inhibition at 0.012mM, reversible and competitive 58898 3.1.3.48 disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate suramin-derivative, 50% inhibition of PTP1B at 0.0096 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58909 3.1.3.48 disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive 58909 3.1.3.48 dithiothreitol complete inhibition at 1.8 mM 45 3.1.3.48 dithiothreitol - 45 3.1.3.48 DNA - 293 3.1.3.48 DTT inhibition of cytosolic enzyme form 177 3.1.3.48 dysidiolide inhibits Cdc25A 138794 3.1.3.48 EDTA 51% inhibition at 5 mM 21 3.1.3.48 ent-17-hydroxykaur-15-en-19-oic acid 40% inhibition at 0.033 mM 231797 3.1.3.48 ent-3beta-angeloyloxykaur-16-en-19-oic acid - 231798 3.1.3.48 ent-3beta-tigloyloxykaur-16-en-19-oic acid - 231799 3.1.3.48 ent-kaur-16-en-19-oic acid diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.020 mM 35063 3.1.3.48 ent-kaur-9(11),16-dien-19-oic acid 29% inhibition at 0.033 mM 231800 3.1.3.48 erybraedin A - 159640 3.1.3.48 erylysins A i.e. 3''-hydroxy-2',2'-dimethylpyrano[6',5':3,4]-2'',2''-dimethyldihydropyrano[6'',5'':9,10]pterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1 159637 3.1.3.48 erylysins B i.e. furano[5',4':3,4]-9-hydroxy-10-prenylpterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1 159638 3.1.3.48 erysubin D - 14891 3.1.3.48 eryvarin D - 14889 3.1.3.48 ethyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoate - 197243 3.1.3.48 ethyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoate - 197249 3.1.3.48 ethyl 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoate - 85217 3.1.3.48 ethyl [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetate - 85216 3.1.3.48 ethyl-3,4-dephostatin - 138790 3.1.3.48 F1S-6C-W11 - 80325 3.1.3.48 Fe2+ 34.5% inhibition at 2 mM 25 3.1.3.48 Fe2+ lung enzyme 25 3.1.3.48 FlAsH the small molecule biarsenical fluorescein derivative, FlAsH, is no inhibitor of the wild-type enzyme but of the engineered WPD insertion mutant enzyme that displays FlAsH-binding cysteine residues. Inhibition of the FlAsH-sensitized TCPTP mutants is rapid and specific, and strong FlAsH sensitivity is observed in mutants that contain as few as two cysteine point mutations in their engineered WPD loops, minimization of FlAsH-binding determinants, overview 159641 3.1.3.48 fluorescein arsenical hairpin binder fluorescein arsenical hairpin binder does not inhibit any wild type PTP, but insertion of a fluorescein arsenical hairpin binder-binding peptide (CCPGCC) at a conserved position in the PTP catalytic-domain's WPD loop confers fluorescein arsenical hairpin binder sensitivity upon divergent PTPs 10149 3.1.3.48 fluoride - 407 3.1.3.48 formaldehyde - 130 3.1.3.48 glycyrrhetic acid - 32238 3.1.3.48 Glyoxal 93% remaining activity at 0.5 mM 1444 3.1.3.48 glyoxalbis(N(4)-methylthiosemicarbazonato)Cu(II) inhibition of protein tyrosine phosphatase activity is the prerequisite for activation of epidermal growth factor receptor by the compound, overview 159647 3.1.3.48 H1-5C-W11 - 80326 3.1.3.48 H2O2 inactivation, phosphate protects, mechanism, overview 22 3.1.3.48 H2O2 the enzyme can be more rapidly inactivated by H2O2 in the absence of EDTA 22 3.1.3.48 H2O2 reversible 22 3.1.3.48 H3VO4 - 2371 3.1.3.48 H3VO4 no effect on PTP-I but PTP-III inhibited 2371 3.1.3.48 H3VO4 slight effect 2371 3.1.3.48 heparin - 227 3.1.3.48 hexadecanoyl-5-hydroxymethyl tetronic acid potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR 36980 3.1.3.48 hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.005 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58907 3.1.3.48 hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.008mM, reversible and competitive 58907 3.1.3.48 hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.0023 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58906 3.1.3.48 hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.0015M, reversible and competitive 58906 3.1.3.48 hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58910 3.1.3.48 hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.020 mM, reversible and competitive 58910 3.1.3.48 hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.0037 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58903 3.1.3.48 hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.007 mM, reversible and competitive 58903 3.1.3.48 hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.0021 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58904 3.1.3.48 hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.0028mM, reversible and competitive 58904 3.1.3.48 hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.0016 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58905 3.1.3.48 hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.002mM, reversible and competitive 58905 3.1.3.48 hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58901 3.1.3.48 hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition at 0.013M, reversible and competitive 58901 3.1.3.48 hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58899 3.1.3.48 hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition at 0.011M, reversible and competitive 58899 3.1.3.48 hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.007 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58900 3.1.3.48 hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.013M, reversible and competitive 58900 3.1.3.48 hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition of PTP1B at 0.00049 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 55883 3.1.3.48 hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate suramin-derivative, 50% inhibition at 0.00009M, reversible and competitive 55883 3.1.3.48 HgCl2 - 110 3.1.3.48 iodoacetate - 93 3.1.3.48 iodoacetic acid - 213 3.1.3.48 iodoacetic acid complete inhibition at 1.0 mM 213 3.1.3.48 ISIS 113715 PTP-1B antisense oligonucleotide ISIS 113715 dose-dependently inhibits PTP-1B mRNA and protein expression, although ISIS 113715 reduces PTP-1B protein levels by greater than 90%, no effects are observed on protein levels of TC-PTPase 25891 3.1.3.48 ISIS 113715 PTP-1B antisense oligonucleotide ISIS 113715 administration reduces PTP-1B mRNA expression in both liver and adipose tissue by 40-50% but does not affect muscle PTP-1B expression 25891 3.1.3.48 isoneorautenol - 14887 3.1.3.48 isopimaric acid modelling of enzyme binding 225607 3.1.3.48 JTT-551 i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview 15003 3.1.3.48 JTT-551 i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in ob/ob mice, overview 15003 3.1.3.48 JTT-551 i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl) ([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in rat L6 cells, overview 15003 3.1.3.48 kanjone - 138792 3.1.3.48 karanjin - 138791 3.1.3.48 L-(+)-Tartrate 6.5% inhibition at 5 mM 15808 3.1.3.48 L-Dopa - 320 3.1.3.48 L-phenylalanine - 104 3.1.3.48 L-Tartrate weak 1874 3.1.3.48 L-Tartrate no inhibition of platelet enzyme 1874 3.1.3.48 L-Tartrate no inhibition of lung enzyme 1874 3.1.3.48 licochalcone E - 166071 3.1.3.48 lithocholic acid natural inhibitor against PTP1B 1325 3.1.3.48 lobaric acid a depsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 159653 3.1.3.48 lupenone isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner 40357 3.1.3.48 lupeol isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner 3130 3.1.3.48 maslinic acid poor inhibition by the isomers 3-epi-maslinic acid and augustic acid 8518 3.1.3.48 maslinic acid - 8518 3.1.3.48 menadione inhibits Cdc25B irreversibly 240 3.1.3.48 methyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoate - 197253 3.1.3.48 methyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoate - 197251 3.1.3.48 methyl (6S,10S)-12-(2-chloro-3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158866 3.1.3.48 methyl (6S,10S)-12-(2-fluoro-5-iodobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158867 3.1.3.48 methyl (6S,10S)-12-(2-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 79023 3.1.3.48 methyl (6S,10S)-12-(3,4-dichlorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 40214 3.1.3.48 methyl (6S,10S)-12-(3,4-difluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158869 3.1.3.48 methyl (6S,10S)-12-(3-bromo-4-fluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 79039 3.1.3.48 methyl (6S,10S)-12-(3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 40237 3.1.3.48 methyl (6S,10S)-12-benzyl-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158871 3.1.3.48 methyl (6S,10S)-12-[(4,6-dichloro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 79040 3.1.3.48 methyl (6S,10S)-12-[(4-chloro-6-fluoro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA, inhibition kinetics, overview 40236 3.1.3.48 methyl (6S,10S)-12-[(5-chloro-1H-indol-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 79018 3.1.3.48 methyl (6S,10S)-12-[(5-methylfuran-2-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate absolutely specific for MptpB, no inhibition of MptpA 79042 3.1.3.48 methyl (6S,10S)-9-hydroxy-12-(3-hydroxybenzyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158872 3.1.3.48 methyl (6S,10S)-9-oxo-12-(pyridin-3-ylmethyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate - 158987 3.1.3.48 methyl 2,4-dihydroxy-6-methylbenzoate isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78934 3.1.3.48 methyl 2-(3-(1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate IC50 of 6.5 mg/ml 197223 3.1.3.48 methyl 2-(3-(1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate IC50 of 9.4 mg/ml 197222 3.1.3.48 methyl 2-[4-[(4-[[ethoxy(oxo)acetyl][2-(methoxycarbonyl)phenyl]amino]-3-ethylphenylalanyl)amino]butoxy]-6-hydroxybenzoate - 138187 3.1.3.48 methyl 3,8-dimethoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78957 3.1.3.48 methyl 3-formyl-2,4-dihydroxy-6-methylbenzoate isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 78958 3.1.3.48 methyl 4,4-dimethyl-3-oxochol-5-en-24-oate - 197242 3.1.3.48 methyl 4-[(benzylseleninyl)methyl]-N-(tert-butoxycarbonyl)-L-phenylalaninate - 158826 3.1.3.48 methyl 5-amino-6-(7-amino-6-methoxy-5,8-dioxo-5,8-dihydroquinolin-2-yl)-4-(2-hydroxy-3,4-dimethoxyphenyl)-3-methylpyridine-2-carboxylate - 63566 3.1.3.48 methyl 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum 79016 3.1.3.48 methyl N-(tert-butoxycarbonyl)-4-(hydroxymethyl)-L-phenylalaninate - 158822 3.1.3.48 methyl N-(tert-butoxycarbonyl)-4-[(5R)-5-(methoxycarbonyl)-9,9-dimethyl-7-oxo-8-oxa-3-thia-2-selena-6-azadec-1-yl]-L-phenylalaninate - 158823 3.1.3.48 methyl oleanolic acid amide - 70812 3.1.3.48 methyl oleanolic acid ester - 70813 3.1.3.48 methyl-5-((3-(benzylcarbamoyl)-6-iodo-4-oxoquinolin-1(4H)-yl)methyl)-2-methoxybenzoate IC50 of more than 20 mg/ml 197219 3.1.3.48 Mg2+ - 6 3.1.3.48 Mn2+ - 11 3.1.3.48 Mn2+ no inhibition of platelet enzyme 11 3.1.3.48 mokko lactone 93.1% PTP1B inhibitory activity with 0.00141 mg/ml 147228 3.1.3.48 molybdate 92.2% inhibition at 5 mM 509 3.1.3.48 molybdate competitive inhibition 509 3.1.3.48 molybdate - 509 3.1.3.48 molybdate no effect on PTP-I, PTP-III inhibited 509 3.1.3.48 additional information overview, development of inhibitors 2 3.1.3.48 additional information overview on recently developed inhibitors 2 3.1.3.48 additional information not inhibitory: okadaic acid 2 3.1.3.48 additional information not inhibitory: pentamidine, okadaic acid, sodium fluoride up to 5 mM, EDTA up to 10 mM 2 3.1.3.48 additional information in absence of externally added Ca2+, no effect of ethylene glycol bis(2-amino-ethylether) N,N,N’,N’-tetracetic acid or trifluoperazine. Not inhibitory: okadaic acid 2 3.1.3.48 additional information inhibition data for isoforms CD45, Cdc25A, VHR; not inhibitory to PTP1B, CD45: disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate 2 3.1.3.48 additional information enzyme is active in unstimulated or thrombin-stimulated platelets. Enzyme is not active in lysate of platelets adherent to fibrinogen 2 3.1.3.48 additional information down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2 2 3.1.3.48 additional information EDTA, sodium tartrate, sodium fluoride, or okadaic acid have no effect on activity 2 3.1.3.48 additional information the presence of the superoxide- and hydrogen peroxide-destroying enzymes superoxide dismutase and catalase has no effect on the rate of the inactivation reaction 2 3.1.3.48 additional information tert-butyl hydroperoxide cumene hydroperoxide do not inactivate PTP1B, 150 nM H2O2 has no measurable effect on enzyme activity 2 3.1.3.48 additional information inhibition of PTP-PEST by RNAi reduces formation of podosomal structures at the cell periphery and reduces bone resorption indicating a positive functional role for this PTP in promoting osteoclast activity 2 3.1.3.48 additional information 3alpha,24,29-trihydroxyolean-12-en-28-oic acid, 3alpha,19alpha-dihydroxyurs-12,20(30)-dien-24,28-dioic acid, and 3alpha,19alpha-dihydroxyurs-12-en-24,28-dioic acid show very weak inhibitory effect towards PTP1B 2 3.1.3.48 additional information beta2AR stimulation on a B cell phosphorylates and inactivates HePTP in a Gs/cAMP/PKA-dependent manner 2 3.1.3.48 additional information not inhibited by costunolide, 11beta,13-dihydrocostunolide, reynosin, 1beta-hydroxy arbusculin A, santamarine, alpha-costol, beta-sitosterol, aplotaxene, and alpha-amyrin stearate 2 3.1.3.48 additional information no inhibition by EDTA at 1 mM 2 3.1.3.48 additional information structure derivatives, derived from papaverine, e.g. Pnu177496, in docking simulations, simulated molecular docking method, overview 2 3.1.3.48 additional information synthesis and inhibitory activity of 38 synthetic chalcones towards PtpA, the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents, structure-activity analysis, overview. No inhibition by 3a, 3b, 3c, 4h, 5l, 6d, 6g, and 6j 2 3.1.3.48 additional information inhibitor synthesis, inhibitor selectivity for PTP1B over TCPTP, overview 2 3.1.3.48 additional information inhibitor synthesis, structure-activity relationships, overview 2 3.1.3.48 additional information inhibitor docking studies with PTP-1B, overview 2 3.1.3.48 additional information interaction between the alpha-cytoplasmic tail of a1beta1 integrin and TCPTP activates TCPTP by disrupting an inhibitory intramolecular bond in TCPTP, screening of screened 64280 small molecules for TCPTP inhibition, overview 2 3.1.3.48 additional information the inhibition mechanism of [RuIII(EDTA)(OH2/OH)]1-/2- shows similar interactions, that may be important in the anti-cancer properties of the active forms of many Ru pro-drugs 2 3.1.3.48 additional information structure-based optimization of benzoic acids as inhibitors of PTPB1 and LMW-PTP, molecular docking study using crystal structures of PTPB1, PDB ID 1G7G and 1XBO, as templates, overview 2 3.1.3.48 additional information hyperosmotic stress inhibits PTP3. Overexpression of a dominant inhibitor of PTP3 leads to constitutive tyrosine phosphorylation and ectopic nuclear localisation of STATc 2 3.1.3.48 additional information synthesis of series of oxovanadium complexes with mixed ligands, a tridentate ONO-donor Schiff base ligand with salicylidene anthranilic acid, and a bidentate NN ligand, e.g., 2,2'-bipyridine, 1,10-phenanthroline, dipyrido[3,2-d:2',3'-f]quinoxaline, dipyrido[3,2-a:2',3'-c]phenazine, or 7-methyldipyrido[3,2-a:2',3'-c]phenazine, spectroscopical analysis, and crystal structures of complexes bound to PTPB1, molecular modeling, overview 2 3.1.3.48 additional information mechanism of substrate selectivity of five bidentate inhibitors, NNY, B07, F6Z, Q1M, and PYN, for PTP1B, compared to SHP-2 and TCPTP, using molecular dynamics simulations and free energy calculations, and crystal structures with PDB IDs 1NNY, 2B07, 2F6Z, 1Q1M, and 1PYN, 1L8k, and 2SHP, overview. Residues Arg24, Arg254, and Gln262 in the second binding site of PTP1B are essential for the high selectivity of inhibitors 2 3.1.3.48 additional information inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibition, overview 2 3.1.3.48 additional information inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibhition, overview 2 3.1.3.48 additional information bis(thiosemicarbazonato) metal complexes, e.g. with Cu2+ or Zn2+, inhibit PTP and its dephophorylating and inhibitory activity on the epidermal growth factor receptor, EGFR 2 3.1.3.48 additional information PTP bidentate inhibitor library synthesis and screening, overview. The bidentate inhibitors have three components: 1. the warheads, alkyne-containing N-phenyloxamic acids that are cell-permeable, potent bioisosteric phosphotyrosine mimics, 2. a variety of different types of building blocks that act as the secondary-site binders, and 3. azide-containing linkers of different lengths joining the warhead and the building blocks, overview 2 3.1.3.48 additional information the substitution of prenyl groups on pterocarpans might be important for in vitro PTP1B inhibitory activity, and hydroxyl group attached to C-6a or an aldehyde group attached to C-8 may decrease this activity. No inhibition by erylysins C, i.e. 8-formyl-3,9-dihydroxy-4,10-diprenylpterocarpan, by cristacarpin, and by erystagallin C 2 3.1.3.48 additional information development of a rapid high-throughput screening method for PTP inhibitors, overview 2 3.1.3.48 additional information design, synthesis and evaluation of a series of bromo-retrochalcones as PTP1B inhibitors based on licochalcone A and E, overview 2 3.1.3.48 additional information design of structure based cyclic peptide inhibitors, synthesis involves a crucial intramolecular transamidation via a ring opening reaction. All the compounds show moderate to good inhibitory activities against MPtpA in micromolar concentrations, enzyme docking study, overview 2 3.1.3.48 additional information the enzyme activity is diminished by increasing acetate buffer ionic strength, but PTP-H2 is unaffected by tetramisole and levamisole, as well as by okadaic acid, sodium fluoride and sodium citrate 2 3.1.3.48 additional information inhibitor design using the crystal structure of PtpA, overview 2 3.1.3.48 additional information not inhibited by H2O2 treatment 2 3.1.3.48 additional information not inhibited by camelliaolean A and camelliaolean B 2 3.1.3.48 additional information shows no sensitivity to H2O2 2 3.1.3.48 additional information structure-based drug design 2 3.1.3.48 additional information IPTG and lactose inhibit the sugar hydrolase activity of the enzyme PTPRdelta 2 3.1.3.48 additional information no autoinhibition 2 3.1.3.48 additional information abietane-type diterpenoids inhibit protein tyrosine phosphatases by stabilizing an inactive enzyme conformation. Abietane-type diterpenoids, a biologically active class of phytometabolites with largely nonpolar structures, are used for the development of pharmaceutically relevant PTP inhibitors. Minor changes in the structures of abietane-type diterpenoids (e.g. the addition of hydrogens) can improve potency (i.e. lower IC50) by several fold. Trodusquemine and benzofuran derivatives bind to C-terminal allosteric sites that attenuate WPD loop dynamics. Mechanisms of inhibition, dynamic docking, modelling, overview 2 3.1.3.48 additional information design and synthesis of azolyl flavonoids as enzyme inhibitors of protein tyrosine phosphatase 1B, molecular modeling and dynamics studies, using the crystal structure of PTP1B (PDB ID 1G1H) reveals the selectivity of triazolyl flavonoid inhibitor 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one for PTP1B over the closely related T-cell protein tyrosine phosphatase (TCPTP), detailed overview. The inhibitory effects and kinetics analysis of the azoyl flavonoids against PTPs are measured, using 4-nitrophenol phosphate as the substrate 2 3.1.3.48 additional information the active sites of PTPs are exceptionally conserved and charged, making it nearly impossible to develop PTP inhibitors that are selective. But targeting PTP protein (substrate/regulatory) interaction sites, which are distal from the active sites, are highly viable and suitable drug targets. Domains outside PTP catalytic domains have also been demonstrated to directly alter PTP activity. Development of drugs that bind to intrinsically disordered regions of the enzyme, overview 2 3.1.3.48 additional information design of non-natural allosteric-inhibition sites in PTPs, in which a tricysteine moiety is engineered within the PTP catalytic domain at a conserved location outside of the active site. Introduction of the tricysteine motif, which does not exist in any wild-type PTP, serves to sensitize target PTPs to inhibition by a biarsenical compound, providing a generalizable strategy for the generation of allosterically sensitized (as) PTPs. Biarsenical reagents as enzyme inhibitors, overview. Enzyme asPTP catalytic domains have differing biarsenical sensitivities, with some being most potently inhibited by biarsenical compounds with large interarsenical distances, whereas others prefer compounds with relatively small interarsenical distances. AsCy3 is an optimized inhibitor of of engineered enzyme asPTP1B 2 3.1.3.48 additional information identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview 2 3.1.3.48 additional information wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate 2 3.1.3.48 additional information 4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives determined as active potent allosteric inhibitors of protein tyrosine phosphatase 1B, in silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents, binding modes and inhibitory mechanism, docking studies, detailed overview 2 3.1.3.48 additional information phosphorylation of PTPN12 at Ser19 changes its substrate interface, and by doing so, selectively decreases its activity toward the human epidermal growth factor receptor 2 (HER2)-pY1196 site, but not other HER2 phosphorylation sites or other known PTPN12 substrates, such as SRC, paxillin, PAK1,VAV2, p130Cas, FAK, and p190RhoGAP 2 3.1.3.48 additional information inhibition of protein tyrosine phosphatase-1B by vanadyl (VO2+) chelates, competitive and noncompetitive inhibition modes, overview 2 3.1.3.48 additional information chemical library screening, kinetic and computational studies of mixed-type inhibitors of protein tyrosine phosphatase 1B, docking and molecular dynamic simulations studies, and enzyme interaction analysis, overview. For the inhibition assays, 4-nitrophenyl phosphate is used as enzyme substrate 2 3.1.3.48 additional information unaffected by EDTA 2 3.1.3.48 additional information unaffected by okadaic acid 2 3.1.3.48 mpV(pic) potent and selective PTP inhibitor, inhibits SPH-1 in a dose-dependent manner 147225 3.1.3.48 MSI-1436 small molecule inhibitor MSI-1436 binds to the disordered C-terminal domain of PTP1B, C-terminal to the catalytic domain, MSI-1436 functions using an allosteric mechanism to direct the enzymatic activity of PTP1B 232722 3.1.3.48 N,1-dibenzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide 41.4% inhibition at 0.02 mg/ml 197215 3.1.3.48 N,1-dibenzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 61.8% inhibition at 0.02 mg/ml 197214 3.1.3.48 N,N'-[benzene-1,4-diylbis(propane-2,2-diylbenzene-4,1-diyl)]bis(1,1,1-trifluoromethanesulfonamide) - 70825 3.1.3.48 N-((4-((E)-2-nitroethenyl)phenyl)carbonyl)glycyl-L-alpha-glutamyl-L-glutamic acid 50% inhibition at 0.0014 mM in absence of 2-mercaptoethanol, at 0.275 mM in presence of 1 mM 2-mercaptoethanol 129697 3.1.3.48 N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide inhibition of enzyme increases caveolin-1 phosphorylation 129705 3.1.3.48 N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide - 58914 3.1.3.48 N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-(4-methylphenyl)acetamide - 63568 3.1.3.48 N-(3-chloro-4-fluorophenyl)-2-[(6,7-dimethoxy-4-oxo-3-phenyl-3,4-dihydro-2-quinazolinyl)sulfanyl]acetamide 80% inhibition at 0.2 mM 231967 3.1.3.48 N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR 58902 3.1.3.48 N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive 58902 3.1.3.48 N-(3-[(3,5-difluorobenzyl)oxy]pyridin-2-yl)-4-pentylbenzenesulfonamide 74% inhibition at 0.2 mM 231986 3.1.3.48 N-(3-[(4-chlorophenyl)sulfanyl]-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide - 63567 3.1.3.48 N-(4-([(6-ethoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide - 158793 3.1.3.48 N-(4-([(6-methoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide - 158817 3.1.3.48 N-(4-([(6-methyl-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide - 158819 3.1.3.48 N-(4-[[(6-nitro-1,3-benzothiazol-2-yl)amino]sulfonyl]-phenyl)acetamide - 158818 3.1.3.48 N-(6-chloro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide - 158821 3.1.3.48 N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzenesulfonamide - 158884 3.1.3.48 N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide - 158820 3.1.3.48 N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-nitrobenzene sulfonamide linear mixed-type inhibition, shows in vivo antihyperglycemic activity 40213 3.1.3.48 N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide - 158870 3.1.3.48 N-(6-fluoro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide - 158812 3.1.3.48 N-(6-methoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide - 158816 3.1.3.48 N-(6-methoxy-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide - 158951 3.1.3.48 N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide - 158813 3.1.3.48 N-(6-methyl-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide linear mixed-type inhibition, shows in vivo antihyperglycemic activity 40216 3.1.3.48 N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide - 158815 3.1.3.48 N-([4-[difluoro(phosphono)methyl]phenyl]acetyl)-a-aspartyl-4-[difluoro(phosphono)methyl]phenylalaninamide - 70814 3.1.3.48 N-1-(2-[(2-oxo-4-propyl-2H-chromen-7-yl)oxy]propanoyl)-3-(trifluoromethyl)benzene-1-sulfonohydrazide 84% inhibition at 0.2 mM 232036 3.1.3.48 N-benzoyl-L-glutamyl-[4-phosphono(difluoromethyl)]-L-phenylalanineamide i.e. BzN-EJJ-amide, 50% inhibition at 4 nM 117576 3.1.3.48 N-benzyl-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide 0.2% inhibition at 0.02 mg/ml; 7.4% inhibition at 0.02 mg/ml 197213 3.1.3.48 N-benzyl-1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide 6.1% inhibition at 0.02 mg/ml 197211 3.1.3.48 n-dodecyl trimethylammonium bromide pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration 129690 3.1.3.48 N-ethylmaleimide both isozymes, 50% inhibition at 7 mM 49 3.1.3.48 N-ethylmaleimide - 49 3.1.3.48 n-hexadecyl trimethylammonium bromide pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration 129692 3.1.3.48 N-Methylmaleimide 76.3% inhibition at 0.5 mM 3354 3.1.3.48 n-tetradecyl trimethylammonium bromide pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration 129691 3.1.3.48 N-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl]-4-tert-butylbenzamide - 85240 3.1.3.48 N-[5-(dimethylamino)-2-hydroxy-3-methoxybenzyl]-N-methyl-2-(4-nitrophenyl)ethanaminium - 63574 3.1.3.48 N-[6-chloro-5-(2,3-dichlorophenoxy)-1-methyl-1H-benzimidazol-2-yl]acetamide 70% inhibition at 0.2 mM 232112 3.1.3.48 N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide mixed-type inhibition, 92% inhibition at 0.2 mM 232113 3.1.3.48 N2-(2-((2-((N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalanyl)amino)ethyl)disulfanyl)ethyl)-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-argininamide in presence of 5-50 nM, 11-35% decrease in cell spreading, 24% decrease in number of migratory cells, dose-dependent increase in Y527 phosphorylation of Src 129703 3.1.3.48 Na+/K+ tartrate 20% residual activity in ovary and 2% residual activity in haemolymph at 10 mM 138789 3.1.3.48 Na3VO4 - 4546 3.1.3.48 NaCl increase in Km-value with increase of ionic strength, 10-fold increase of Km-value from 0 to 200 mM NaCl 42 3.1.3.48 NaCl inhibits activity with 4-nitrophenyl phosphate 42 3.1.3.48 NaCl inhibits the catalytic domain by 60% at 2 M 42 3.1.3.48 NaF 1 mM, 85% residual activity 235 3.1.3.48 NaF moderate inhibition, both SynPPP1 and SYnPPM3 235 3.1.3.48 NaF 16% residual activity in ovary and no activity in haemolymph at 10 mM 235 3.1.3.48 NaF weak 235 3.1.3.48 NaF - 235 3.1.3.48 NaF no inhibition of platelet enzyme 235 3.1.3.48 NaF no inhibition of lung enzyme 235 3.1.3.48 NaF slight inhibition 235 3.1.3.48 NAT6-297775 - 71556 3.1.3.48 Ni2+ - 38 3.1.3.48 NO inactivation, phosphate protects 277 3.1.3.48 nocardione A inhibits Cdc25B 138795 3.1.3.48 nocardione B inhibits Cdc25B 138796 3.1.3.48 NSC-87877 potent Shp2 and Shp1 inhibitor 71557 3.1.3.48 o-vanadate both SynPPP1 and SYnPPM3 6136 3.1.3.48 o-vanadate Na3VO4, complete inhibition at 0.6 mM 6136 3.1.3.48 okadaic acid both SynPPP1 and SYnPPM3 720 3.1.3.48 okadaic acid complete inhibition of enzyme isolated from metacyclic stage, 35% inhibition of enzyme from procyclic stage 720 3.1.3.48 okadaic acid 7.5% inhibition at 0.01 mM 720 3.1.3.48 oleanolic acid - 2975 3.1.3.48 oleanolic acid amide - 70895 3.1.3.48 oleanolic alcohol - 70896 3.1.3.48 oleanonic acid - 36219 3.1.3.48 orientanol C - 159639 3.1.3.48 orthovanadate 50% inhibition at 0.075 mM 1328 3.1.3.48 orthovanadate inhibition of protein tyrosine phosphatase activity 1328 3.1.3.48 orthovanadate 24.5% inhibition at 5 mM 1328 3.1.3.48 orthovanadate - 1328 3.1.3.48 orthovanadate competitive inhibitor 1328 3.1.3.48 p-chloromercuribenzoate lung enzyme 43 3.1.3.48 p-hydroxymercuribenzoate - 98 3.1.3.48 p-nitrocatechol sulfate competitive inhibitor 4040 3.1.3.48 PAO complete inhibition at 0.0.5 mM 60568 3.1.3.48 papaverine binding structure, molecular modeling, overview 1540 3.1.3.48 paracaseolide A - 197181 3.1.3.48 peracetic acid a potent, time-dependent inactivator of the catalytic subunit of PTP1B, treatment of the enzyme with 0.015 mM for 15 sec inactivates 88% of the enzyme, inactivation of PTP1B by peracetic acid can be reversed by treatment of the enzyme with thiols 4679 3.1.3.48 pervanadate pervanadate inhibits PTP by irreversibly oxidizing the catalytic cysteine of PTP 9619 3.1.3.48 pervanadate - 9619 3.1.3.48 phaseollin - 14888 3.1.3.48 phenyl vinyl sulfonate phenyl vinyl sulfonate-mediated PTP inactivation is active site-directed and irreversible 147224 3.1.3.48 phenyl vinyl sulfone phenyl vinyl sulfone-mediated PTP inactivation is active site-directed and irreversible 35475 3.1.3.48 Phenylarsine oxide 55.8% inhibition at 0.01 mM 2031 3.1.3.48 Phenylarsine oxide specific inhibitor of protein Tyr phosphatase activity 2031 3.1.3.48 Phenylarsine oxide a specific PTP inhibitor, 79% inhibition at 1.0 nM 2031 3.1.3.48 Phenylarsine oxide - 2031 3.1.3.48 phenylhydrazonopyrazolone sulfonate 1 potent, active site-directed small molecule inhibitor which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B 18801 3.1.3.48 phenylhydrazonopyrazolone sulfonate 4 the most potent inhibitor of Shp2 which shows a specificity profile similar to phenylhydrazonopyrazolone sulfonate 1 147230 3.1.3.48 phosphate competitive 16 3.1.3.48 phosphate 38% residual activity in ovary and 3% residual activity in haemolymph at 10 mM 16 3.1.3.48 phosphate inhibits the phosphatase activity, but not the sugar hydrolase activity; inhibits the phosphatase activity, but not the sugar hydrolase activity 16 3.1.3.48 phosphate - 16 3.1.3.48 phosphotyrosine - 2579 3.1.3.48 PO43- treatment of the enzyme with 0.05 mM PO43- for 15 sec inactivates 49% of the enzyme 867 3.1.3.48 PO43- - 867 3.1.3.48 poly(Glu-Tyr) - 20808 3.1.3.48 pomolic acid - 71559 3.1.3.48 potassium bisperoxo(1,10-phenanthroline)oxovanadate - 24986 3.1.3.48 potassium bisperoxo(1,10-phenanthroline)oxovanadate complete inhibition at 0.01 mM 24986 3.1.3.48 potassium bisperoxo(1,10-phenanthroline)oxovanadate potent PTP inhibitor 24986 3.1.3.48 potassium bisperoxo(1,10-phenanthroline)oxovanadate(V) i.e. [bpV(phen)], the peroxovanadium compound is a stable, potent and selective protein tyrosine phosphatase inhibitor. It protects dorsal column sensory axons and white matter and rescues sensory-evoked potentials in vivo after treatement with PTP or spinal cord injury, overview 159648 3.1.3.48 propanal 93% remaining activity at 0.5 mM 328 3.1.3.48 pterokaurene L3 no inhibition at 0.031 mM 232129 3.1.3.48 regucalcin regulatory protein in intracellular signaling 35449 3.1.3.48 rilobolide-6-O-methacrylate no inhibition at 0.026 mM 232130 3.1.3.48 RK-682 - 11931 3.1.3.48 RK-682 98.5% PTP1B inhibitory activity with 0.0012 mg/ml 11931 3.1.3.48 rotungenic acid - 71558 3.1.3.48 S-nitrosoglutathione S-nitrosoglutathione treatment decreases the catalytic activity parameters of PtpA by half 980 3.1.3.48 SK7 a metal chalcone, complete inhibition at 0.02 mM 232712 3.1.3.48 small t antigen small t antigen of DNA tumor virus SV40 inhibits the phosphatase activity of the PP2A core enzyme 24971 3.1.3.48 SO42- - 245 3.1.3.48 sodium decylsulfate at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects 129688 3.1.3.48 Sodium diphosphate both isoforms, inhibition by millimolar concentrations 2669 3.1.3.48 sodium dodecylsulfate at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects 1066 3.1.3.48 Sodium fluoride NaF, 30% inhibition at 5 mM, no inhibition at 1-3 mM 2758 3.1.3.48 Sodium fluoride 96% inhibition at 2 mM 2758 3.1.3.48 sodium octylsulfate at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects 129689 3.1.3.48 sodium ortho-vanadate - 132706 3.1.3.48 sodium orthovanadate - 3399 3.1.3.48 sodium orthovanadate both isozymes, 50% inhibition at 3 mM 3399 3.1.3.48 sodium orthovanadate complete inhibition of enzyme isolated from metacyclic stage, 30% inhibition of enzyme from procyclic stage 3399 3.1.3.48 sodium orthovanadate 20% residual activity in ovary and 13% residual activity in haemolymph at 0.1 mM 3399 3.1.3.48 sodium orthovanadate shows dose-dependent inhibition of PRL activity 3399 3.1.3.48 sodium orthovanadate 17.5% inhibition at 1 mM 3399 3.1.3.48 sodium orthovanadate a broad-range PTP inhibitor, abrogated Cr(VI)-induced clonogenic lethality 3399 3.1.3.48 sodium orthovanadate strong inhibition 3399 3.1.3.48 sodium orthovanadate 99.5% inhibition at 0.05 mM 3399 3.1.3.48 sodium pervanadate broad-acting tyrosine phosphatase inhibitor 147226 3.1.3.48 Sodium tetradecylsulfate at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects 30412 3.1.3.48 sodium tungstate complete inhibition of enzyme isolated from metacyclic stage, 50% inhibition of enzyme from procyclic stage 23741 3.1.3.48 Sodium vanadate 1 mM, 60-80% inhibition 4598 3.1.3.48 Sodium vanadate - 4598 3.1.3.48 Sodium vanadate a PTP inhibitor targeting the catalytic site pocket. Vanadate is anchored in the active site of Tk-PTP(form II), stabilized by electrostatic interaction with the guanidinium group of Arg109 and by its oxygen atom-mediated hydrogen bonds with the main chain amides of Met94, Gly95, Leu97, Gly98, and Arg99. The Tk-PTP(form II) P-loop is structurally similar to those of catalytically active DUSP proteins 4598 3.1.3.48 sorbitol - 1149 3.1.3.48 spathodic acid - 71561 3.1.3.48 spermidine - 148 3.1.3.48 spermine 2.0-20 mM 197 3.1.3.48 stevastelin inhibits VHR; inhibits VHR; inhibits VHR 36979 3.1.3.48 stigmasterol - 2584 3.1.3.48 sulfircin inhibits Cdc25A 138793 3.1.3.48 suramin 50% inhibition of PTP1B at 0.011 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 704 3.1.3.48 suramin 50% inhibition at 0.007M, reversible and competitive 704 3.1.3.48 suramin - 704 3.1.3.48 taraxerol - 25242 3.1.3.48 Tartrate both SynPPP1 and SYnPPM3 762 3.1.3.48 tetrachyrin - 232161 3.1.3.48 tetramisole both SynPPP1 and SYnPPM3 34600 3.1.3.48 tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate suramin-derivative, 50% inhibition of PTP1B at 0.00025 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 35451 3.1.3.48 tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate suramin-derivative, 50% inhibition at 0.0007mM, reversible and competitive 35451 3.1.3.48 tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR 58912 3.1.3.48 tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive 58912 3.1.3.48 tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate suramin-derivative, 50% inhibition of PTP1B at 0.08 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58913 3.1.3.48 tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate suramin-derivative, 50% inhibition at 0.045 mM, reversible and competitive 58913 3.1.3.48 tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate suramin-derivative, 50% inhibition of PTP1B at 0.0045 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58908 3.1.3.48 tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate suramin-derivative, 50% inhibition at 0.005mM, reversible and competitive 58908 3.1.3.48 tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR 58911 3.1.3.48 tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate suramin-derivative, 50% inhibition at 0.0042 mM, reversible and competitive 58911 3.1.3.48 Trifluoperazine complete inhibition of enzyme isolated from metacyclic stage, 18% inhibition of enzyme from procyclic stage 977 3.1.3.48 trilobolide-6-O-isobutyrate no inhibition at 0.026 mM 232162 3.1.3.48 tungstate 16.3% inhibition at 20 mM 1989 3.1.3.48 tungstate competitive inhibition 1989 3.1.3.48 tungstate - 1989 3.1.3.48 ursolic acid 50% inhibition at 0.0038 mM, competitive inhibition 2291 3.1.3.48 ursolic acid - 2291 3.1.3.48 ursolic acid 99% PTP1B inhibitory activity with 0.0007 mg/ml 2291 3.1.3.48 uvaol - 71562 3.1.3.48 vanadate - 233 3.1.3.48 vanadate competitive, 1 mM, 11% residual activity 233 3.1.3.48 vanadate enzyme inhibition by vanadate takes place through an oxidant-independent pathway, the inhibition is reversible with EDTA 233 3.1.3.48 vanadate the equatorial vanadate oxygen atoms bind to the P-loop and assumes a trigonal bipyramidal geometry in both transition state analogue structures, with very similar apical O-O distances, binding structure, overview 233 3.1.3.48 VO3N3 oxovanadium(IV) is coordinated with one nitrogen and two oxygen atoms from the Schiff base and two nitrogen atoms from the bidentate planar ligands, in a distorted octahedral geometry, VO3N3 159636 3.1.3.48 wedelolide D 32% inhibition at 0.020 mM 232164 3.1.3.48 wedelolide H no inhibition at 0.023 mM 232165 3.1.3.48 wedelolide I no inhibition at 0.021 mM 232166 3.1.3.48 wedelolide J no inhibition at 0.021 mM 232167 3.1.3.48 Zn2+ 75.2% inhibition at 5 mM 14 3.1.3.48 Zn2+ Zn2+ inhibits the enzyme irreversibly in a concentration-dependent manner 14 3.1.3.48 Zn2+ - 14 3.1.3.48 Zn2+ strong inhibition 14 3.1.3.48 Zn2+ low nanomolar Zn2+ concentrations inhibit isoform PTB1Bll 14 3.1.3.48 Zn2+ 65.5% inhibition at 2.5 mM 14 3.1.3.48 [(1-benzyl-1H-indazol-5-yl)(difluoro)methyl]phosphonic acid - 79097 3.1.3.48 [(2-benzyl-2H-indazol-5-yl)(difluoro)methyl]phosphonic acid - 79100 3.1.3.48 [(4-bromophenyl)(difluoro)methyl]phosphonic acid - 79114 3.1.3.48 [(4-[(4E)-2-(1H-benzotriazol-1-yl)-2-[4-(methoxycarbonyl)phenyl]-5-phenylpent-4-en-1-yl]phenyl)(difluoro)methyl]phosphonic acid - 138189 3.1.3.48 [(4-[[3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid - 79098 3.1.3.48 [(4-[[4-bromo-3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid selectivity with different PTPs, overview 79116 3.1.3.48 [(4-[[4-bromo-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid - 79212 3.1.3.48 [(4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid - 79117 3.1.3.48 [(BzMeIm)Au(I)Cl] - 159646 3.1.3.48 [(MeIm)Au(I)Cl] - 159643 3.1.3.48 [(MeMeIm)Au(I)Cl] - 159644 3.1.3.48 [(p-MeBzMeIm)Au(I)Cl] - 159645 3.1.3.48 [2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid irreversible inhibition 232172 3.1.3.48 [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetic acid - 85218 3.1.3.48 [biphenyl-4-yl(difluoro)methyl]phosphonic acid - 79282 3.1.3.48 [difluoro(4-nitrophenyl)methyl]phosphonic acid - 79276 3.1.3.48 [difluoro(4-[[2-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid - 79283 3.1.3.48 [difluoro(4-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid - 79227 3.1.3.48 [difluoro(4-[[4-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid - 79278 3.1.3.48 [difluoro(4-[[4-fluoro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid - 79279 3.1.3.48 [difluoro[3-(phenylcarbamoyl)phenyl]methyl]phosphonic acid - 78887 3.1.3.48 [difluoro[4-(1,3-thiazol-2-ylcarbamoyl)phenyl]methyl]phosphonic acid - 79281 3.1.3.48 [difluoro[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]phosphonic acid - 79192 3.1.3.48 [difluoro[4-(methylcarbamoyl)phenyl]methyl]phosphonic acid - 78985 3.1.3.48 [difluoro[4-(phenoxymethyl)phenyl]methyl]phosphonic acid - 79035 3.1.3.48 [difluoro[4-(phenylcarbamoyl)phenyl]methyl]phosphonic acid - 79288 3.1.3.48 [difluoro[4-(phenylsulfamoyl)phenyl]methyl]phosphonic acid - 79289 3.1.3.48 [difluoro[4-(propan-2-ylcarbamoyl)phenyl]methyl]phosphonic acid - 79287 3.1.3.48 [RuIII(EDTA)(OH2/OH)]1-/2- RuIII-EDTA inhibits PTP, like vanadate, through an oxidant-independent pathway. It inhibits PTP at physiological pH values by a mechanism that involves binding of the Cys residue of the catalytic domain of the enzyme, overview. At pH 7.4, the Ru-EDTA complex exists as a mixture of aqua and hydroxo-species. The inhibition is reversible or inhibited by glutathione 159635 3.1.3.48 [[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid - 232178 3.1.3.48 [[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid - 78982 3.1.3.48 [[4-(1H-benzimidazol-2-ylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid - 158896 3.1.3.48 [[4-(benzoylamino)phenyl](difluoro)methyl]phosphonic acid - 79099 3.1.3.48 [[4-(benzylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid - 79108 3.1.3.48 [[4-([[3,5-bis(trifluoromethyl)phenyl]carbamoyl]amino)phenyl](difluoro)methyl]phosphonic acid - 79119 3.1.3.48 [[4-[(1-ethylpiperidin-4-yl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79109 3.1.3.48 [[4-[(2-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79047 3.1.3.48 [[4-[(2-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79107 3.1.3.48 [[4-[(3-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79112 3.1.3.48 [[4-[(3-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79113 3.1.3.48 [[4-[(4-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79030 3.1.3.48 [[4-[(4-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid - 79111