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MDL-800

Chemical Structure : MDL-800

CAS No.: 2275619-53-7

MDL-800 (MDL800)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 626.289
Formula C21H16BrCl2FN2O6S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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

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