2.7.11.10 (1R,4R)-4-(2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanol - 254288 2.7.11.10 (4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid IC50 for the IKKbeta is 0.0022 mM 57755 2.7.11.10 (E)-2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol the compound directly binds to the ATP binding site of the enzyme with a strong binding affinity 256714 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-2-(but-1-oxy)-4-(2-methoxyethoxymethoxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells 146817 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-2-(hexyl-1-oxy)-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function 146819 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-2-ethoxy-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid - 146821 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(pentyl-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid - 146823 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-en-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid - 146824 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-yn-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells 146818 2.7.11.10 (E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-phenylmethoxy-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function 146820 2.7.11.10 (E)-4-[3-(5-adamant-1-yl-4-(2-methoxyethoxymethoxy)-2-(prop-1-oxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid - 146822 2.7.11.10 (R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 254640 2.7.11.10 (R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 254641 2.7.11.10 (S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 254709 2.7.11.10 1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide - 254765 2.7.11.10 1-(4-chlorophenyl)-4-ureido-1H-pyrazole-3-carboxamide i.e. SC-108 172147 2.7.11.10 1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea inhibits IKK with IC50 of 0.02 mM 57738 2.7.11.10 1-(benzo[d][1,3]dioxol-5-yl)-8-(3-chloroisonicotinamido)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide i.e. PHA-379 172148 2.7.11.10 1-(benzo[d][1,3]dioxol-5-yl)-8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-4,5-dihydro-1H-benzo-[g]indazole-3-carboxamide i.e. PHA-250 172149 2.7.11.10 1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline-6,7-diol NCI0288748, 65% inhibition at 0.1 mM 254874 2.7.11.10 1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine - 39799 2.7.11.10 1-[4-(1-hydroxynaphthalen-2-yl)-6-imino-3-methyl-6,7-dihydropyrazolo[3,4-d][1,3]thiazin-1(4H)-yl]-2-phenylethan-1-one NCI0657381, 76% inhibition at 0.1 mM 254905 2.7.11.10 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine - 39800 2.7.11.10 1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide - 39798 2.7.11.10 1088 P protein - 213597 2.7.11.10 15d-prostaglandin J2 strongly inhibits IKK 127412 2.7.11.10 17-acetoxyjolkinolide B 17-AJB is isolated from a traditional Chinese medicinal herb Euphorbia fischeriana Steud. 17-AJB interacts with IKK directly and keeps IKK in its phosphorylated form irreversibly, inactivating its kinase activity, leading to its failure to activate NF-kappaB. The effect of 17-AJB on IKK is specific. It has no effect on other kinases such as p38, p44/42, and JNK. 17-AJB induces apoptosis in tumor cells 71084 2.7.11.10 2,4-diamino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 220678 2.7.11.10 2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide - 254987 2.7.11.10 2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzamide - 254988 2.7.11.10 2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine - 39837 2.7.11.10 2-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid IC50 for the IKK complex is above 0.1 mM 57754 2.7.11.10 2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255160 2.7.11.10 2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255161 2.7.11.10 2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide - 255162 2.7.11.10 2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255163 2.7.11.10 2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255164 2.7.11.10 2-amino-4-(2-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]- pyrimidine-5-carbonitrile - 255165 2.7.11.10 2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255166 2.7.11.10 2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255167 2.7.11.10 2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255168 2.7.11.10 2-amino-4-(2-morpholinoethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255169 2.7.11.10 2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255171 2.7.11.10 2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255172 2.7.11.10 2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255173 2.7.11.10 2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255174 2.7.11.10 2-amino-4-(4-(2-hydroxyethyl)piperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255175 2.7.11.10 2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255176 2.7.11.10 2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255177 2.7.11.10 2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255178 2.7.11.10 2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile - 255179 2.7.11.10 2-amino-4-(4-methylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255180 2.7.11.10 2-amino-4-(4-phenylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255181 2.7.11.10 2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255182 2.7.11.10 2-amino-4-(cyclohexyl(2-hydroxyethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255183 2.7.11.10 2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255184 2.7.11.10 2-amino-4-(cyclohexylmethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile - 255185 2.7.11.10 2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255186 2.7.11.10 2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255187 2.7.11.10 2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255188 2.7.11.10 2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255189 2.7.11.10 2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255190 2.7.11.10 2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile - 255191 2.7.11.10 2-amino-6-(2-hydroxy-6-isobutoxyphenyl)-4-(piperidin-3-yl)nicotinonitrile i.e. PHA-535E 172143 2.7.11.10 2-benzamido-pyrimidines diverse derivatives, synthesis and inhibitory potential determination, overview 127417 2.7.11.10 2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide - 77477 2.7.11.10 2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39825 2.7.11.10 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide BMS-066, inhibitor of IKKbeta 12064 2.7.11.10 2-[[bis(2-hydroxyethyl)amino]methyl]-4-(2-methylbutan-2-yl)phenol NCI0079692, 59% inhibition at 0.1 mM 255306 2.7.11.10 3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide - 255339 2.7.11.10 3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide - 255340 2.7.11.10 3-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid IC50 for the IKKbeta is 0.001 mM 57753 2.7.11.10 3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide - 77481 2.7.11.10 3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide - 77489 2.7.11.10 3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide - 77487 2.7.11.10 3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide - 77494 2.7.11.10 3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide - 77496 2.7.11.10 3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide - 77485 2.7.11.10 3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide - 77488 2.7.11.10 3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide - 77484 2.7.11.10 3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide - 77503 2.7.11.10 3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide - 77506 2.7.11.10 3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide - 77502 2.7.11.10 3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide - 77486 2.7.11.10 3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77520 2.7.11.10 3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77500 2.7.11.10 3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77497 2.7.11.10 3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77521 2.7.11.10 3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77501 2.7.11.10 3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77504 2.7.11.10 3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 27085 2.7.11.10 3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77498 2.7.11.10 3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77522 2.7.11.10 3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77511 2.7.11.10 3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 27088 2.7.11.10 3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77513 2.7.11.10 3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77512 2.7.11.10 3-amino-6-(4-hydroxy-3,3-dimethylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 155487 2.7.11.10 3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77505 2.7.11.10 3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 27086 2.7.11.10 3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77507 2.7.11.10 3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77510 2.7.11.10 3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide - 77483 2.7.11.10 3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide - 77493 2.7.11.10 3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide - 77492 2.7.11.10 3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77482 2.7.11.10 3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide - 77491 2.7.11.10 3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide - 77490 2.7.11.10 3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide - 77495 2.7.11.10 3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide - 77480 2.7.11.10 3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide - 27087 2.7.11.10 3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide - 77499 2.7.11.10 3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77519 2.7.11.10 3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77517 2.7.11.10 3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77518 2.7.11.10 3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77516 2.7.11.10 3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77509 2.7.11.10 3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77508 2.7.11.10 3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide - 77515 2.7.11.10 3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide - 27084 2.7.11.10 3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile - 77475 2.7.11.10 3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide - 39794 2.7.11.10 3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide - 39796 2.7.11.10 4'-amino-4-chloro-4''-sulfamoyl-1,1':3',1''-terphenyl-5'-carboxamide - 155482 2.7.11.10 4,8-dimethoxy-1-vinyl-beta-carboline i.e. beta-carboline alkaloid C-1, isolated from Melia azedarach var. japonica, inhibits IKK activity by reduction of IKK phosphorylation and degradation, and activation and nuclear translocation of NF-kappaB and subsequent signalling pathways 127416 2.7.11.10 4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide - 255525 2.7.11.10 4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzoic acid - 255526 2.7.11.10 4-(1-benzothiophen-2-yl)-N-[3-chloro-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 250 nM 57564 2.7.11.10 4-(1-benzothiophen-2-yl)-N-[3-methoxy-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 150 nM 57565 2.7.11.10 4-(1-benzothiophen-2-yl)-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 0.0085 mM, cellular profile 57558 2.7.11.10 4-(1-benzothiophen-2-yl)-N-[4-([4-(dimethyl-amino)piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 80 nM, cellular profile 57562 2.7.11.10 4-(1-benzothiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 70 nM, cellular profile 57563 2.7.11.10 4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline BMS-345541, inhibitor of IKKbeta 27076 2.7.11.10 4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide - 255535 2.7.11.10 4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide - 255536 2.7.11.10 4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide - 255537 2.7.11.10 4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide - 255538 2.7.11.10 4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide - 255539 2.7.11.10 4-(5-(3-acetamino-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 800 nM 57569 2.7.11.10 4-(5-(3-amino-3-ethylpentyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 30 nM 57570 2.7.11.10 4-(5-(3-amino-3-methyl-but-1-ynyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 200 nM 57568 2.7.11.10 4-(5-(3-amino-3-methyl-butyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 40 nM 57758 2.7.11.10 4-(5-(3-hydroxy-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amin IC50 for the IKK complex is 50 nM, cellular profile 57757 2.7.11.10 4-(5-(3-methoxypropyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 100 nM, cellular profile 57567 2.7.11.10 4-(5-(4-hydroxybutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine IC50 for the IKK complex is 40 nM, cellular profile 57566 2.7.11.10 4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide - 255553 2.7.11.10 4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide - 39808 2.7.11.10 4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide - 255560 2.7.11.10 4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine - 255564 2.7.11.10 4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid IC50 for the IKK complex is 0.018 mM, cellular profile 57752 2.7.11.10 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine - 255593 2.7.11.10 4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 77469 2.7.11.10 4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39824 2.7.11.10 4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 77467 2.7.11.10 4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 77470 2.7.11.10 4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39831 2.7.11.10 4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39830 2.7.11.10 4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 77468 2.7.11.10 4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39829 2.7.11.10 4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39826 2.7.11.10 4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39828 2.7.11.10 4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 77471 2.7.11.10 4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine - 39827 2.7.11.10 4-[6-[(2-hydroxyethyl)amino]-7-methyl-7,8-dihydro-2H,6H-[1,3]dioxolo[4,5-g][1]benzopyran-8-yl]-2,6-dimethoxyphenol NCI0671177, 68% inhibition at 0.1 mM 255654 2.7.11.10 4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide - 39795 2.7.11.10 4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide - 39813 2.7.11.10 4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide - 39812 2.7.11.10 4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide - 39815 2.7.11.10 4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide - 39797 2.7.11.10 4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide - 39806 2.7.11.10 4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide NCI0107328, 94% inhibition at 0.1 mM 255661 2.7.11.10 5,6-dibromo-beta-carboline inhibits IKK with IC50 of 600 nM 57748 2.7.11.10 5-((3-fluorophenyl)ethynyl)-2-ureidothiophene-3-carboxamide i.e. PHA-966 172145 2.7.11.10 5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide i.e. SC-440 172144 2.7.11.10 5-amino-2,30-bithiophene-4-carboxamide i.e. SC-514 172146 2.7.11.10 5-Aminosalicylate weak inhibition of IKK-2 3607 2.7.11.10 5-bromo-6-chloro-beta-carboline inhibits IKK with IC50 of 600 nM 57749 2.7.11.10 5-bromo-6-cyano-beta-carboline inhibits IKK with IC50 of 0.0011 mM 57751 2.7.11.10 5-bromo-6-fluoro-beta-carboline inhibits IKK with IC50 of 0.002 mM 57747 2.7.11.10 5-bromo-6-methoxy-beta-carboline nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM 57745 2.7.11.10 5-bromo-6-trifluoromethyl-beta-carboline inhibits IKK with IC50 of 0.0011 mM 57750 2.7.11.10 5-bromo-beta-carboline inhibits IKK with IC50 of 0.015 mM 57746 2.7.11.10 6,6-dimethyl-1-[3-[3-(3-nitrophenoxy)propoxy]phenyl]-1,3,5-triazinane-2,4-diimine NCI0111727, 75% inhibition at 0.1 mM 255740 2.7.11.10 6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline inhibits IKK with IC50 of 0.003 mM 57744 2.7.11.10 6,8-dichloro-7-ethoxy-9H-beta-carboline inhibits IKK with IC50 of 140 nM 57741 2.7.11.10 6,8-dichloro-7-methoxy-9H-beta-carboline inhibits IKK with IC50 of 170 nM 57740 2.7.11.10 6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate inhibits IKK with IC50 of 0.0032 mM 57743 2.7.11.10 6,8-dichloro-beta-carboline inhibits IKK with IC50 of 200 nM 57556 2.7.11.10 6-bromo-7-(piperidin-4-yloxy)isoquinoline - 39802 2.7.11.10 6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline - 39803 2.7.11.10 6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline - 39811 2.7.11.10 6-phenyl-7-(piperidin-3-yloxy)isoquinoline - 39810 2.7.11.10 6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline - 39814 2.7.11.10 6-phenyl-7-(piperidin-4-yloxy)isoquinoline - 39801 2.7.11.10 6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline - 39818 2.7.11.10 6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline - 39819 2.7.11.10 7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 77472 2.7.11.10 7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 77473 2.7.11.10 7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 77474 2.7.11.10 7-(3-[[2-(3,5-dihydroxyphenyl)-2-hydroxyethyl]amino]propyl)-1,3-dimethyl-8-(morpholin-4-yl)-3,7-dihydro-1H-purine-2,6-dione NCI0293897, 55% inhibition at 0.1 mM 255798 2.7.11.10 7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 27081 2.7.11.10 7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline inhibits IKK with IC50 of 80 nM 57742 2.7.11.10 7-(piperidin-4-yloxy)isoquinoline - 39809 2.7.11.10 7-hydroxy-6,8-dichloro-beta-carboline inhibits IKK with IC50 of 0.011 mM 57557 2.7.11.10 7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline - 39804 2.7.11.10 7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline - 39805 2.7.11.10 7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 77476 2.7.11.10 7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline - 39817 2.7.11.10 7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline - 39807 2.7.11.10 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide PHA-408, ATP-competitive, selective IKK-2 inhibitor; PHA-408, ATP-competitive, selective IKK-2 inhibitor 12065 2.7.11.10 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide PHA-408, ATP-competitive, selective IKK-2 inhibitor 12065 2.7.11.10 8-amino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0013 mM 57722 2.7.11.10 8-dimethylamino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0018 mM 57724 2.7.11.10 8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine - 39834 2.7.11.10 8-methylamino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0018 mM 57723 2.7.11.10 8-nitro-6-chloro-beta-carboline inhibits IKK with IC50 of 0.004 mM 57721 2.7.11.10 acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] - 39835 2.7.11.10 Acetylsalicylate weak inhibition of IKK-2 4779 2.7.11.10 Acetylsalicylic acid nonspecific for IKK, anti-inflammatory 2261 2.7.11.10 antirheumatic gold compound inhibition of IKKbeta 135574 2.7.11.10 arsenic trioxide nonspecific for IKK, acts on a cystein ersidue in the activation loop 13269 2.7.11.10 arsenite inhibition of IKKbeta 397 2.7.11.10 AS602868 IKKbeta inhibitor 17790 2.7.11.10 AS602868 - 17790 2.7.11.10 AS602868 inhibitor of IKK-beta 17790 2.7.11.10 Bay 11-7082 - 57759 2.7.11.10 Berberine an isoquinoline alkaloid derived from a plant used traditionally in Chinese and Ayurvedic medicine inhibits IKK activity. Addition of DTT to the kinase reaction reverses the berberine-mediated inhibition of IKK activity 1612 2.7.11.10 BI605906 an IKKbeta inhibitor 172141 2.7.11.10 BMS-345541 specific for IKK-2, binds at an allosteric site 127418 2.7.11.10 BMS345541 shows efficacy in a mouse model of collagen-induced arthritis without signs of major toxicology 146816 2.7.11.10 BX795 - 77523 2.7.11.10 chalcone - 3804 2.7.11.10 chrysin chrysin interacts weakly with the I-kappa-B kinase epsilon binding site and inhibits the enzyme at doses higher than 0.06 mM 1727 2.7.11.10 COMPOUND A leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth 146009 2.7.11.10 curcumin weak inhibition of IKK-2 696 2.7.11.10 cyclopentenone prostaglandins nonspecific for IKK, anti-inflammatory 35184 2.7.11.10 cyclopentenone prostaglandins inhibition of IKKbeta 35184 2.7.11.10 cyclopentenone prostanoids inhibition of IKK and thus inhibition of NFkappaB-mediated HSV-1-induced HIV-1 replication 127414 2.7.11.10 cyclopentone prostaglandines inhibition of IKK-2 127419 2.7.11.10 DDTC - 135575 2.7.11.10 ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl] - 39836 2.7.11.10 evodiamine alkaloid extracted from Evodia rutaecarpa fruits exhibiting antiproliferative, antimetastatic, and apoptotic activities, inhibits IKKalpha activity, suppresses IKKalpha phosphorylation and degradation, and specifically blocks NF-kappaB activation by IKK and other agents, translocation, and activity, overview 35183 2.7.11.10 IMD-0354 in macrophages, the inhibition of IkappaB kinase beta (IKKbeta) results in lower proinflammatory cytokine expression caused by heat-killed Helicobacter pylori cells. Treatment with IKKbeta inhibitor results in milder inflammation in gerbils with Helicobacter pylori gastritis 25835 2.7.11.10 IMD-0354 - 25835 2.7.11.10 IMD-0354 specific IKKbeta inhibition 25835 2.7.11.10 LY294002 phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not 770 2.7.11.10 lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide NCI0339925, 93% inhibition at 0.1 mM 255949 2.7.11.10 methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate inhibits IKK with IC50 of 700 nM 57737 2.7.11.10 methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate - 77514 2.7.11.10 additional information CREB-binding protein-bound NEMO/IKKgamma inhibits IKKalpha and p65 transcriptional activities 2 2.7.11.10 additional information evodiamine analogue rutaecarpine does not inhibit IKK and NF-kappaB activation 2 2.7.11.10 additional information simvastatin inhibits the TNFalpha-induced activation of IkappaB kinase and activation of NF-kappaB in vitro and in vivo, simvastatin highly affects the whole NF-kappaB-dependent pathway of signaling, overview 2 2.7.11.10 additional information prolyl hydroxylase-1 negatively regulates IKKbeta, hydroxylation represses IKKbeta activity by altering protein expression or by preventing its activation through phosphorylation on S177/S181 2 2.7.11.10 additional information two structurally unrelated kinase inhibitors, termed NG25 or 5Z-7-oxozeaenol, inhibit the TAK1 protein kinase, and therefore also inhibit activation of IKKalpha and IKKbeta 2 2.7.11.10 additional information structure-based design of IKK-2 inhibitors based on induced-fit docking into the homology model, overview 2 2.7.11.10 MRT67307 an IKKepsilon/TBK1 kinase inhibitor 172142 2.7.11.10 MX781 0.02 mM inhibit IKKbeta by 65% in the presence of an ATP concentration corresponding to its Km value 146010 2.7.11.10 N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine - 27080 2.7.11.10 N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine - 39823 2.7.11.10 N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine - 27079 2.7.11.10 N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine - 27077 2.7.11.10 N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine - 27078 2.7.11.10 N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine - 39816 2.7.11.10 N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine - 39820 2.7.11.10 N-(2-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide IC50 for the IKK complex is 0.0044 mM 57756 2.7.11.10 N-(2-dimethyl-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide IC50 for the IKK complex is 300 nM, cellular profile 57559 2.7.11.10 N-(2-pyrrolidin-1-yl-ethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide IC50 for the IKK complex is 500 nM 57561 2.7.11.10 N-(3,5-bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide - 155488 2.7.11.10 N-(3-methyl-butyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide IC50 for the IKKbeta is above 0.1 mM 57560 2.7.11.10 N-(3-[2-imino-6-methyl-3-[(3-nitrophenyl)methyl]-4-oxo-1,2,3,4-tetrahydropyrimidin-5-yl]propyl)-4-methylbenzene-1-sulfonamide NCI0211135, complete inhibition at 0.1 mM 256034 2.7.11.10 N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide - 256036 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide inhibits IKK with IC50 of 0.003 mM 57729 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide inhibits IKK with IC50 of 0.02 mM 57732 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide inhibits IKK with IC50 of 600 nM 57733 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide inhibits IKK with IC50 of 0.02 mM 57727 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide inhibits IKK with IC50 of 0.0013 mM 57734 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)acetamide inhibits IKK with IC50 of 600 nM 57726 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)benzamide inhibits IKK with IC50 of 700 nM 57728 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide inhibits IKK with IC50 of 0.02 mM 57736 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide inhibits IKK with IC50 of 0.0083 mM 57735 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide inhibits IKK with IC50 of 0.02 mM 57739 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide inhibits IKK with IC50 of 0.001 mM 57730 2.7.11.10 N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide inhibits IKK with IC50 of 300 nM 57731 2.7.11.10 N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine - 39821 2.7.11.10 N-acetylcysteine inhibits phosphorylation of IkappaBalpha 3479 2.7.11.10 N-benzyl-6-chloro-9H-beta-carbolin-8-amine inhibits IKK with IC50 of 0.02 mM 57725 2.7.11.10 N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine - 39833 2.7.11.10 N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine - 39832 2.7.11.10 N-tosyl-L-phenylalanine chloromethyl ketone - 5193 2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide - 27083 2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide - 27082 2.7.11.10 N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide - 77479 2.7.11.10 N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide - 39822 2.7.11.10 N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide - 39838 2.7.11.10 N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide - 39839 2.7.11.10 N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide - 39843 2.7.11.10 N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide - 39840 2.7.11.10 N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide - 39842 2.7.11.10 N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide - 39841 2.7.11.10 N1-(1,8-dimethylimidazo-[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine i.e. PHA-068E 172150 2.7.11.10 N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide - 77478 2.7.11.10 N2-(2-chlorophenyl)-N-[6-[(2-chlorophenyl)sulfamoyl]-2-methyl-4-oxoquinazolin-3(4H)-yl]glycinamide NCI0687760, 89% inhibition at 0.1 mM 256228 2.7.11.10 N4-cyclohexyl-5-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine - 256240 2.7.11.10 N4-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine - 256241 2.7.11.10 NBD peptide NEMO-binding domain peptide 155490 2.7.11.10 nimbolide nimbolide inhibits TNF-alpha-induced p65 nuclear translocation and phosphorylation. Nimbolide binds to and inhibits IKK activation. It suppresses NF-betaB activation by inhibition of IkappaBbeta kinase, wild-type not IKKbeta mutant C179A, leading to suppression of IkappaBalpha phosphorylation and degradation, nuclear translocation, DNA binding, and gene transcription 172140 2.7.11.10 noraristeromycin NAM 5392 2.7.11.10 PHA-408 selective IKK-2 inhibitor 39844 2.7.11.10 PHA-408 a selective IKK-2 inhibitor, shows time-dependent binding to the enzyme 39844 2.7.11.10 prostaglandin 2alpha inhibits IKK 127413 2.7.11.10 prostaglandin A1 strongly inhibits IKK 3093 2.7.11.10 Prostaglandin A2 strongly inhibits IKK 5607 2.7.11.10 prostaglandin E1 inhibits IKK 1654 2.7.11.10 prostaglandin E2 inhibits IKK 913 2.7.11.10 protein HSCARG or NMRAL1, NmrA-like family domain-containing protein 1, inhibits the phosphorylation of IKKbeta 155489 2.7.11.10 PS-1145 i.e. 8-(NHC(O)-3'-pyridyl)-6-chloro-beta-carboline, inhibits IKK with IC50 of 100 nM in vitro, blocks phosphorylation of IkappaBalpha and subsequent activation of NFkappaB in vivo 57720 2.7.11.10 PS1145 inhibits IKK, blocks TNFalpha activation by IKK in vivo 127415 2.7.11.10 Rapamycin suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex; suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex 4862 2.7.11.10 ring finger protein 8 upon TNFalpha stimulation, ring finger protein 8 binds to the catalytic subunits of the enzyme complex, resulting in inhibition of IkappaB kinase alpha/beta phosphorylation and subsequent nuclear factor-kappaB activation 256711 2.7.11.10 RNAi specific IKKbeta inhibition 1580 2.7.11.10 S1627 specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview 35182 2.7.11.10 S1627 preferentially inhibits the beta-subunit of the IKK complex. Specific inhibition of I-kappaB kinase by S1627 modulates the nociceptive response in various nociceptive models in rats. S1627 inhibits the activation of NF-kappaB in the spinal cord and thereby thermal and mechanical hyperalgesia in the zymosan-induced paw inflammation model and the inflammatory edema. It also reduces tactile and cold allodynia in a model of neuropathic pain 35182 2.7.11.10 salicylate weak inhibition of IKK-2 617 2.7.11.10 SC-514 i.e. 4-amino-[2,3'-bithiophene]-5-carboxamide 256713 2.7.11.10 shRNA - 4411 2.7.11.10 sulfasalazine weak inhibition of IKK-2 4146 2.7.11.10 sulfasalazine nonspecific for IKK, anti-inflammatory 4146 2.7.11.10 sulindac sulfide nonspecific for IKK, anti-inflammatory 3533 2.7.11.10 tetrandrine a bis-benzylisoquinoline alkaloid isolated from the roots of Han-Fang-Ji (Stephania Tetrandra S Moore) effectively inhibits IKKs phosphorylation 25834 2.7.11.10 TPCA-1 - 256712 2.7.11.10 TPCA-1 i.e. 5-[(4-fluorophenyl)-2-ureido]thiophene-3-carboxamide 256712 2.7.11.10 trans-resveratrol nonspecific for IKK, anti-inflammatory 11594 2.7.11.10 vaccina virus virulence factor B14 interacts and inhibits IKKcomplex. Interaction between vaccina virus virulence factor B14 and IKK complex requires IKKbeta but not IKKalpha 146825 2.7.11.10 vaccinia virus virulence factor B14 interacts and inhibits IKKcomplex. Interaction between B14 and IKK complex requires IKKbeta but not IKKalpha 146814 2.7.11.10 Wortmannin phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not 631 2.7.11.10 YopJ effector protein YopJ from Yersinia pestis inhibits MAPK kinase and IKK activation by acetylating the conserved serine and threonine residues in the activation loop of the kinase. Furthermore, YopJ inhibits Tax-mediated IkappaB phosphorylation 146815