MDL-800 | Allosteric activator of SIRT6
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 50 mg | $315.00 | ||
| 10 mg | $85.00 |
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:
- Huang et al. (2018) Identification of a cellularly active SIRT6 allosteric activator; Chem. Biol. 14 1118
- Chen et al. (2020) The SIRT6 activator MDL-800 improves genomic stability and pluripotency of old murine-derived iPS cells; Aging Cell 19 e13185
- 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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:
- Huang et al. (2018) Identification of a cellularly active SIRT6 allosteric activator; Chem. Biol. 14 1118
- Chen et al. (2020) The SIRT6 activator MDL-800 improves genomic stability and pluripotency of old murine-derived iPS cells; Aging Cell 19 e13185
- 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
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