MDL-800 | Allosteric Inhibitor of SIRT6

MDL-800 (2275619-53-7) is an allosteric activator of SIRT6 (EC50 = 10.3 µM).1 It specifically activates the deacetylase (H3K9ac and H3K56ac) activity of SIRT6 – inactive against SIRT1,3,4 and HDACs 1-11 with 10x less activity against SIRT2,5,7. It inhibited the growth of human hepatocarcinoma cells (HCC) via the tumor suppressor deacetylase (H3K9ac and H3K56ac) via cell-cycle arrest and showed efficacy in a xenograft model of HCC.  MDL-800 improved the genetic stability of old-murine-derived iPSCs via activation of NHEJ and BER DNA repair pathways suggesting promise in treating age-related diseases via iPSC-based therapies.2 MDL-800 inhibited the proliferation of 12 non-small cell lung carcinoma cell lines with IC50 values of 21.5 to 34.5 µM.3 It also enhanced the effects of EGFR kinase inhibitors in Osimertinib-resistant HCC827 and PC9 cells as well as in patient-derived primary tumor cells.3

References:

  1. Huang et al. (2018) Identification of a cellularly active SIRT6 allosteric activator; Chem. Biol. 14 1118
  2. Chen et al. (2020) The SIRT6 activator MDL-800 improves genomic stability and pluripotency of old murine-derived iPS cells; Aging Cell 19 e13185
  3. Shang et al. (2021) MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer; Acta Pharmacol. Sin. 42 120
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

10 mg, 50 mg

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CAS:
2275619-53-7
Catalog Number:
10-4415
Activity:
Allosteric inhibitor of SIRT6
Chemical Names:
Methyl 2-(N-(5-Bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-(3,5-dichlorophenylsulfonamido)benzoate
Molecular Weight:
626.29
Molecular Formula:
C21H16BrCl2FN2O6S2
Solubility:
Soluble in DMSO (up to at least 10 mg/ml with warming)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

MDL-800 | Allosteric Inhibitor of SIRT6

$85.00$315.00

CAS:
2275619-53-7
Catalog Number:
10-4415
Activity:
Allosteric inhibitor of SIRT6
Chemical Names:
Methyl 2-(N-(5-Bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-(3,5-dichlorophenylsulfonamido)benzoate
Molecular Weight:
626.29
Molecular Formula:
C21H16BrCl2FN2O6S2
Solubility:
Soluble in DMSO (up to at least 10 mg/ml with warming)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
  • 10 mg
  • 50 mg
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