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Chemical Structure : MDL-811
Catalog No.: PC-20269Not For Human Use, Lab Use Only.
MDL-811 (MDL811) is a potent, selective and allosteric SIRT6 activator with EC50 of 5.7 uM (activated SIRT6 deacetylation), two-fold greater activity than MDL-800 (EC50=12.3 uM, Cat# 35760).
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MDL-811 (MDL811) is a potent, selective and allosteric SIRT6 activator with EC50 of 5.7 uM (activated SIRT6 deacetylation), two-fold greater activity than MDL-800 (EC50=12.3 uM, Cat# 35760).
MDL-811 shows little effect on other histone deacetylase (HDAC) enzymes.
MDL-811 shows significantly enhanced bioavailability (F%, 92.96%) compared with MDL-800 (71.33%).
MDL-811 significantly enhances the deacetylation of SIRT6 (H3K9Ac, H3K18Ac, and H3K56Ac) in natural nucleosomes and HEK293T cells in a dose-dependent manner.
MDL-811 exhibits broad antiproliferative effects on CRC cells (IC50=4.7-61 uM), binds and stabilize SIRT6 in CRC cells, reduces histone H3 acetylation through the activation of SIRT6 deacetylase activity.
MDL-811 (30 mg/kg, i.p.) exhibits robust anti-tumor efficacy in CRC CDX and PDX models, inhibits tumorigenesis in the APCmin/+ model of spontaneous CRC.
MDL-811 suppresses CYP24A1 gene transcription, enhances the anti-tumor activity of vitamin D3 in CRC.
| M.Wt | 681.41 | |
| Formula | C25H25BrCl2FN3O5S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jialin Shang, et al. Theranostics. 2020 Apr 27;10(13):5845-5864.
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