EC Number   |
Inhibitors |
Structure |
|---|
   2.3.1.B41 | quercetin |
38% inhibition at 0.1 mM |
   |
| 2.3.1.B41 | Cl316,243 |
a lipolysis drug, interfers with SIRT6 |
|
| 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 |
|
| 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 |
|
| 2.3.1.B41 | more |
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 |
|
| 2.3.1.B41 | nicotinamide |
inhibits the deacetylation of native histones much more effectively than deacetylation of a synthetic substrate |
|
| 2.3.1.B41 | H2N-AK-(N(epsilon)-thioacetyl-)lysine-LM-COOH |
moderate potent inhibitor |
|
| 2.3.1.B41 | H2N-HK-(N(epsilon)-thioacetyl-)lysine-LM-COOH |
moderate potent inhibitor |
|
| 2.3.1.B41 | more |
nicotinamide insensitivity, IC50: 2.1 mM |
|
| 2.3.1.B41 | more |
not inhibited by linoleic acid, oleic acid, oleoylethanolamide, and myristoylethanolamide |
|
