2.3.1.B41 (4R)-1-[(benzyloxy)carbonyl]-4-hydroxy-L-prolyl-N6-ethanethioyl-N-phenyl-L-lysinamide 0.2 mM, 56% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196340 2.3.1.B41 (9H-fluoren-9-yl)methyl(6-acetamido-1-(dodecylamino)-1-oxohexan-2-yl)carbamate - 245404 2.3.1.B41 (9H-fluoren-9-yl)methyl(6-acetamido-1-(dodecylamino)-1-oxohexanyl) carbamate - 247434 2.3.1.B41 1-(4,5-dihydropyrrolo[1,2-a]quinoxalin-4-yl)naphthalen-2-ol - 245472 2.3.1.B41 1-(tert-butoxycarbonyl)-L-prolyl-N6-ethanethioyl-N-phenyl-L-lysinamide 0.2 mM, 32% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196341 2.3.1.B41 2,4-dioxo-N-(4-(pyridin-3-yloxy)phenyl)-1,2,3,4-tetrahydroquinazoline-6-sulfonamide i.e. compound Q, a SIRT6 inhibitor with quinazolinedione-like structure, which reduces both SIRT6 deacetylase and deacylase activities 247435 2.3.1.B41 2,6-diamino-N-dodecylhexanamide - 245520 2.3.1.B41 2,6-diamino-N-octadecylhexanamide - 245521 2.3.1.B41 2-acetamido-6-amino-N-octadecylhexanamide - 245631 2.3.1.B41 2-acetamido-6-amino-N-tetradecylhexanamide - 247433 2.3.1.B41 3-morpholinosydnonimine - 8305 2.3.1.B41 4-phenyl-4,5-dihydropyrrolo[1,2-a]quinoxaline - 246041 2.3.1.B41 4-phenyl-5-((3-(trifluoromethyl)phenyl)sulfonyl)-4,5-dihydropyrrolo[1,2-a]quinoxaline - 246042 2.3.1.B41 4-phenyl-5-(phenylsulfonyl)-4,5-dihydropyrrolo[1,2-a]quinoxaline - 246043 2.3.1.B41 5-(phenylsulfonyl)-4-(pyridin-3-yl)-4,5-dihydropyrrolo[1,2-a]quinoxaline - 246145 2.3.1.B41 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide i.e. EX-527. 0.2 mM, 56% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196745 2.3.1.B41 Cl316,243 a lipolysis drug, interfers with SIRT6 247436 2.3.1.B41 H2N-AK-(N(epsilon)-thioacetyl-)lysine-LM-COOH moderate potent inhibitor 212793 2.3.1.B41 H2N-HK-(N(epsilon)-thioacetyl-)lysine-LM-COOH moderate potent inhibitor 212792 2.3.1.B41 luteolin 30% inhibition at 0.1 mM 436 2.3.1.B41 methyl N2-acetyl-N6-ethanethioyl-L-lysyl-L-alaninate 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196337 2.3.1.B41 additional information splitomicin and sirtinol fail to inhibit PfSir2 2 2.3.1.B41 additional information nicotinamide insensitivity, IC50: 2.1 mM 2 2.3.1.B41 additional information not inhibited by linoleic acid, oleic acid, oleoylethanolamide, and myristoylethanolamide 2 2.3.1.B41 additional information preparation of the 4-substituited-4,5-dihydropyrrolo[1,2-a]quinoxalines and 4-substituited-pyrrolo[1,2-a]quinoxalines 2 2.3.1.B41 additional information identification of SIRT6 inhibitors that decrease SIRT6 deacetylase activity and evoke coherent biological effects in cells. These inhibitors include a family of compounds with a quinazolinedione-based structure and a family of compounds with salicylate-based structure, with an IC50 for the SIRT6-catalyzed deacetylase activity in the low micromolar range. Relative enzyme activity in presencee of inhibitors compared to control, overview. No inhibition by (9H-fluoren-9-yl)methyl [(2S)-6-[(tert-butoxycarbonyl)amino]-1-(dodecylamino)-1-oxohexan-2-yl]carbamate and tert-butyl [(5S)-5-acetamido-6-(dodecylamino)-6-oxohexyl]carbamate 2 2.3.1.B41 N,N'-(6-(octadecylamino)-6-oxohexane-1,5-diyl)diacetamide - 246530 2.3.1.B41 N-[(5S)-5-acetamido-6-(dodecylamino)-6-oxohexyl]-N,N-dimethylmethanaminium - 246760 2.3.1.B41 N2-acetyl-N-dodecyl-L-lysinamide - 246840 2.3.1.B41 N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-(2-fluorophenyl)-L-lysinamide 0.2 mM, 25% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196335 2.3.1.B41 N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-pyridin-3-yl-L-lysinamide 0.2 mM, 54% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196343 2.3.1.B41 N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-[2-(4-methoxyphenyl)-2-oxoethyl]-L-lysinamide 0.2 mM, 48% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amino-4-methylcoumarin 196342 2.3.1.B41 N6-ethanethioyl-N-(2-oxo-2-phenylethyl)-N2-(3-phenylpropanoyl)-L-lysinamide 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196338 2.3.1.B41 N6-ethanethioyl-N-phenyl-N2-[3-(pyridin-3-yl)propanoyl]-L-lysinamide 0.2 mM, 18% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196339 2.3.1.B41 N6-ethanethioyl-N2-(3-phenylpropanoyl)-L-lysyl-L-alanine 0.2 mM, 20% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 196336 2.3.1.B41 N6-ethanethioyl-N2-[3-(2-fluorophenyl)propanoyl]-N-pyridin-3-yl-L-lysinamide 0.2 mM, 58% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amino-4-methylcoumarin 196344 2.3.1.B41 nicotinamide inhibits the deacetylation of native histones much more effectively than deacetylation of a synthetic substrate 267 2.3.1.B41 quercetin 0.2 mM, 52% inhibition, substrate: Ac-RYQ(N6-acetyl)K-7-amido-4-methylcoumarin 137 2.3.1.B41 quercetin 38% inhibition at 0.1 mM 137 2.3.1.B41 tert-butyl (5-acetamido-6-(octadecylamino)-6-oxohexyl)carbamate - 246940 2.3.1.B41 tert-butyl (5-amino-6-(dodecylamino)-6-oxohexyl)carbamate - 246941 2.3.1.B41 tert-butyl (5-amino-6-(octadecylamino)-6-oxohexyl)carbamate - 246942 2.3.1.B41 trichostatin A TSA, a potent, zinc-chelating hydroxamate inhibitors of zinc-dependent deacylases, which potently and isoform-specifically inhibits Sirt6. Sirtuin 6 inhibition mechanism, structural basis and interaction analysis, detailed overview. The binding site are nicotinamide pocket and acyl channel, binding kinetics 1314