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首页-小分子抑制剂&激动剂-Epigenetics-Sirtuin -MDL-811
MDL-811

Chemical Structure : MDL-811

CAS No.: 2275619-98-0

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MDL-811 (MDL811)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 681.41
    分子式 C25H25BrCl2FN3O5S2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (R)-N-(5-bromo-4-fluoro-2-methylphenyl)-4-((3,5-dichlorophenyl)sulfonamido)-2-((3-methylmorpholino)methyl)benzenesulfonamide

    参考文献

    1. Jialin Shang, et al. Theranostics. 2020 Apr 27;10(13):5845-5864.

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