2.3.1.286 (4R)-1-(tert-butoxycarbonyl)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 83.4% inhibition 196318 2.3.1.286 (4R)-1-(tert-butoxycarbonyl)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide 0.05 mM, 97.1% inhibition 196320 2.3.1.286 (4R)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 89.3% inhibition 196319 2.3.1.286 (4R)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide 0.05 mM, 96.8% inhibition 196321 2.3.1.286 (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 10% inhibition at 0.05 mM 196302 2.3.1.286 (5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 17% inhibition at 0.05 mM; 20% inhibition at 0.05 mM 196301 2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM 196307 2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 25% inhibition at 0.05 mM 196306 2.3.1.286 (5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 22% inhibition at 0.05 mM 196305 2.3.1.286 (5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 41% inhibition at 0.05 mM 196299 2.3.1.286 (7aS,12aS)-7-(4-chlorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 5% inhibition at 0.05 mM 212784 2.3.1.286 (7aS,12aS)-7-(4-methoxyphenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 38% inhibition at 0.05 mM 212785 2.3.1.286 (7aS,12aS)-7-phenyl-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 18% inhibition at 0.05 mM 212783 2.3.1.286 (7aS,12aS)-7-[4-(thiophen-2-yl)phenyl]-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 16% inhibition at 0.05 mM 212786 2.3.1.286 (7aS,12aS)-9-bromo-7-(4-chlorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 50% inhibition at 0.05 mM 212789 2.3.1.286 (7aS,12aS)-9-bromo-7-(4-fluorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 65% inhibition at 0.05 mM 212788 2.3.1.286 (7aS,12aS)-9-bromo-7-(4-methoxyphenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 65% inhibition at 0.05 mM 212790 2.3.1.286 (7aS,12aS)-9-bromo-7-phenyl-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 70% inhibition at 0.05 mM 212787 2.3.1.286 (7aS,12aS)-9-bromo-7-[4-(furan-2-yl)phenyl]-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline about 78% inhibition at 0.05 mM 212791 2.3.1.286 1-(tert-butoxycarbonyl)prolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 93.7% inhibition 196316 2.3.1.286 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)isonicotinamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196769 2.3.1.286 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)isonicotinamide selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196761 2.3.1.286 2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate i.e. Ro 31-8220; i.e. Ro 31-8220; i.e. Ro 31-8220 196746 2.3.1.286 3-((2-methoxynaphthalen-1-yl)methyl)-7-((2-methylbenzyl)amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196773 2.3.1.286 3-((2-methoxynaphthalen-1-yl)methyl)-7-((pyridin-3-ylmethyl)amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one i.e. ICL-SIRT078, a substrate-competitive SIRT2 inhibitor with more than 50fold selectivity against SIRT1, 3 and 5. Treatment of MCF-7 breast cancer cells with ICL-SIRT078 results in hyperacetylation of alpha-tubulin, an established SIRT2 biomarker, at doses comparable with the biochemical IC50 data, while suppressing MCF-7 proliferation at higher concentrations 196771 2.3.1.286 3-((2-methoxynaphthalen-1-yl)methyl)-7-((thiophen-2-ylmethyl)-amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196774 2.3.1.286 3-((2-methoxynaphthalen-1-yl)methyl)-7-(neopentylamino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196777 2.3.1.286 3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196326 2.3.1.286 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-chlorophenyl)benzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3 196754 2.3.1.286 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196755 2.3.1.286 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(5-chloropyridin-2-yl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 196766 2.3.1.286 3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-(4-chloro-2-fluorophenyl)-N-methylbenzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196758 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfinyl)phenyl)benzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3 196750 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfonyl)phenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196751 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196760 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 196752 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-cyanopyridin-2-yl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 196765 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-fluoropyridin-2-yl)benzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 196749 2.3.1.286 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(6-chloropyridazin-3-yl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 196764 2.3.1.286 3-(N-(5-chloropyridin-2-yl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196757 2.3.1.286 3-acetylpyridine 16.8% inhibition at 30 mM 3783 2.3.1.286 3-bromopyridine 19.1% inhibition at 30 mM 163975 2.3.1.286 3-chloropyridine 9% inhibition at 30 mM 48594 2.3.1.286 3-fluoropyridine less than 2% inhibition at 30 mM 163982 2.3.1.286 3-hydroxypyridine 83.9% inhibition at 15 mM 13128 2.3.1.286 3-methoxypyridine 10.8% inhibition at 30 mM 232528 2.3.1.286 3-pyridine-carboxyaldehyde 10.6% inhibition at 30 mM 232527 2.3.1.286 3-Pyridinemethanol 22.5% inhibition at 30 mM 15539 2.3.1.286 4-bromo-N-(3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)phenyl)benzamide selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196762 2.3.1.286 5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 14% inhibition at 0.05 mM 196300 2.3.1.286 5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 196310 2.3.1.286 5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 20% inhibition at 0.05 mM 196303 2.3.1.286 5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 196312 2.3.1.286 5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 196304 2.3.1.286 5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 13% inhibition at 0.05 mM 196311 2.3.1.286 5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 196309 2.3.1.286 5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione - 196308 2.3.1.286 5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione 30% inhibition at 0.05 mM 196298 2.3.1.286 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EX-527; i.e. EX-527; i.e. EX-527 196745 2.3.1.286 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - 196745 2.3.1.286 7-((3-fluorobenzyl)amino)-3-((2-methoxynaphthalen-1-yl)methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196775 2.3.1.286 7-((3-methoxybenzyl)amino)-3-((2-methoxynaphthalen-1-yl)-methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196776 2.3.1.286 7-(benzylamino)-3-((2-methoxynaphthalen-1-yl)methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one - 196772 2.3.1.286 acetyl-protamine - 232529 2.3.1.286 alpha-1-O-methyl-adenosine diphosphoribose - 232530 2.3.1.286 Benzamide 5% inhibition at 5 mM 1408 2.3.1.286 Benzamide 44% inhibition at 5 mM 1408 2.3.1.286 cambinol - 196737 2.3.1.286 coumermycin A1 completely inhibited by 0.2 mM 190443 2.3.1.286 EX-527 - 212779 2.3.1.286 Ex257 specific inhibitor of isoform SIRT1 212777 2.3.1.286 fisetin - 1257 2.3.1.286 Isonicotinamide weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro; weak inhibitor 12567 2.3.1.286 Isonicotinamide 4% inhibition at 5 mM 12567 2.3.1.286 Isonicotinamide 18% inhibition at 5 mM 12567 2.3.1.286 Isonicotinamide 5% inhibition at 42 mM 12567 2.3.1.286 macrocyclic peptide inhibitor S2iL5 the inhibitor binds to the active site of SIRT2 through extensive interactions. The inhibitor induces an open-to-closed domain movement and a helix-to-coil transition in a SIRT2-specific region 196747 2.3.1.286 meta-azi-propofol only binds specifically and competitively to the enzyme when co-equilibrated with other substrates 212782 2.3.1.286 methyl N2-(tert-butoxycarbonyl)-N6-ethanethioyl-L-lysyl-D-alaninate 0.05 mM, 81.3% inhibition 196315 2.3.1.286 additional information no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220 2 2.3.1.286 additional information not inhibited by benzamide 2 2.3.1.286 N-(3-(N-(4-chlorophenyl)-N-methylsulfamoyl)phenyl)-4-cyanobenzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 196763 2.3.1.286 N-(4-acetylphenyl)-3-(N-(4-acetylphenyl)-N-methylsulfamoyl)benzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 196767 2.3.1.286 N-(4-bromo-2-fluorophenyl)-3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-methylbenzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 196759 2.3.1.286 N-(4-chlorophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 196768 2.3.1.286 N-(4-cyanophenyl)-3-(N-(4-(1-hydroxyethyl)phenyl)-N-methylsulfamoyl)benzamide - 196770 2.3.1.286 N-(4-cyanophenyl)-3-(N-(4-fluorophenyl)-N-methylsulfamoyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196748 2.3.1.286 N-(4-cyanophenyl)-3-(N-(4-methoxyphenyl)-N-methylsulfamoyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 196753 2.3.1.286 N-(4-cyanophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 196756 2.3.1.286 N-methyl-N-nitrosourea - 26019 2.3.1.286 N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-5-oxoprolinamide 0.05 mM, 98.2% inhibition 196322 2.3.1.286 N-[(2S)-6-(ethanethioylamino)-1-[[2-(morpholin-4-yl)ethyl]amino]-1-oxohexan-2-yl]-6-oxoheptanamide 0.05 mM, 61.1% inhibition 196324 2.3.1.286 N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(4-methoxyphenyl)-2-oxoethyl]-L-lysinamide 0.05 mM, 95.6% inhibition 196314 2.3.1.286 N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide 0.05 mM, 37.5% inhibition 196313 2.3.1.286 N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide 0.05 mM, 54.9% inhibition 196325 2.3.1.286 N6-ethanethioyl-N2-(6-oxoheptanoyl)-N-(2-oxo-2-phenylethyl)-L-lysinamide 0.05 mM, 97.7% inhibition 196323 2.3.1.286 nicotinamide - 267 2.3.1.286 nicotinamide mixed noncompetitive inhibitor. Inhibition of SIRT3 involves apparent competition between the inhibitor and the enzyme cofactor NAD+; predominantly noncompetitive inhibitor 267 2.3.1.286 nicotinamide 0.5 mM, complete inhibition 267 2.3.1.286 nicotinamide noncompetitive inhibitor versus NAD+ 267 2.3.1.286 nicotinamide noncompetitive inhibitor versus NAD+. 95% inhibition at 1.5 mM 267 2.3.1.286 nicotinamide noncompetitive inhibitor 267 2.3.1.286 nicotinic acid 18.3% inhibition at 15 mM 1282 2.3.1.286 o-phenanthroline - 239 2.3.1.286 poly-L-arginine - 45840 2.3.1.286 prolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 94.8% inhibition 196317 2.3.1.286 propofol only binds specifically and competitively to the enzyme when co-equilibrated with other substrates 1898 2.3.1.286 Pyrazinamide 4% inhibition at 5 mM 3666 2.3.1.286 Pyrazinamide 1% inhibition at 5 mM 3666 2.3.1.286 Pyridine 6.4% inhibition at 30 mM 2033 2.3.1.286 resveratrol inhibits deacetylase activity 799 2.3.1.286 sirtinol 24% inhibition at 0.05 mM 196736 2.3.1.286 sirtinol - 196736 2.3.1.286 splitomicin - 75552 2.3.1.286 suramin - 704 2.3.1.286 tenovin-1 - 212778 2.3.1.286 tenovin-6 - 212780 2.3.1.286 Thionicotinamide 4% inhibition at 5 mM 8199 2.3.1.286 Thionicotinamide 16% inhibition at 5 mM 8199 2.3.1.286 Thionicotinamide 15% inhibition at 5 mM 8199 2.3.1.286 Thionicotinamide 58.3% inhibition at 15 mM 8199 2.3.1.286 [histone H3]-difluoroacetyl-L-lysine - 232525 2.3.1.286 [histone H3]-monofluoroacetyl-L-lysine - 232524 2.3.1.286 [histone H3]-thioacetyl-L-lysine most potent inhibitor 232523 2.3.1.286 [histone H3]-trifluoroacetyl-L-lysine - 232526