Chemical Structure : MDL-800
CAS No.: 2275619-53-7
Catalog No.: 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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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.
M.Wt | 626.289 | |
Formula | C21H16BrCl2FN2O6S2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-((3,5-dichlorophenyl)sulfonamido)benzoate |
1. Huang Z, et al. Nat Chem Biol. 2018 Oct 29. doi: 10.1038/s41589-018-0150-0.
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