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首页-小分子抑制剂&激动剂-Epigenetics-Sirtuin -MDL-800
MDL-800

Chemical Structure : MDL-800

CAS No.: 2275619-53-7

MDL-800 (MDL800)

货号: PC-35760Not For Human Use, Lab Use Only.

MDL-800 (MDL800) is a first-in-class, selective, cellular active SIRT6 allosteric activator, increases SIRT6 deacetylation activity with EC50 of 10.3 uM in RHKK-ac-AMC and FDL assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MDL-800 (MDL800) is a first-in-class, selective, cellular active SIRT6 allosteric activator, increases SIRT6 deacetylation activity with EC50 of 10.3 uM in RHKK-ac-AMC and FDL assays.
MDL-800 dramatically enhanced SIRT6 deacetylation activity by more than 22-fold, displays no activity toward SIRT1, SIRT3, SIRT4, and HDAC1-11 at 50-100 uM, as well as >10-fold selectivity toward SIRT2, SIRT5, and SIRT7.
MDL-800activates SIRT6 through a surface allosteric site induces H3K9ac and H3K56ac deacetylation and represses proliferation of HCC cells (IC50=23.3 uM).
MDL-800 inhibits xenograft tumor growth of HCC cells in immunocompromised mice by activating the deacetylase activity of SIRT6.

物理化学性质&存储条件

分子量 626.289
分子式 C21H16BrCl2FN2O6S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-((3,5-dichlorophenyl)sulfonamido)benzoate

参考文献

1. Huang Z, et al. Nat Chem Biol. 2018 Oct 29. doi: 10.1038/s41589-018-0150-0.

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