货号 | 2780/50 |
别名 | 6-Chloro-2,3,4,9-tetrahydro-1H-carb |
供应商 | Tocris |
生物活性 | Selective inhibitor of SIRT1 that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members (IC50 values are 98, 19600, 48700, > 100000 and > 100000 nM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Enhances p53 acetylation in response to DNA damaging agents. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 248.71 |
分子式 | C13H13ClN2O |
可溶性/溶解性 | Soluble to 75 mM in DMSO and to 50 mM in ethanol |
CAS号 | 49843-98-3 |
参考文献 | Zhaoet al (2013) The 2.5 Å crystal structure of the SIRT1 catalytic domain bound to nicotinamide adenine dinucleotide (NAD+) and an indole (EX527 analogue) reveals a novel mechanism of histone deacetylase inhibition. J.Med.Chem. 56 963. PMID: 23311358. Solomonet al (2006) Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol.Cell.Biol. 26 28. PMID: 16354677. Napperet al (2005) Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J.Med.Chem. 48 8045. PMID: 16335928. |