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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-MI-238
MI-238

Chemical Structure : MI-238

CAS No.: 883801-00-1

MI-238 (MI 238)

货号: PC-49852Not For Human Use, Lab Use Only.

MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.

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

    生物&药学活性

    MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.
    MI-238 is docked into Mcl-1 BH3 binding groove and proximal to the BH1 domain of Mcl-1.
    MI-238 disrupts Bak/Mcl-1 interaction in a dose-dependent manner in vitro, directly binds to Mcl-1 and inhibits Mcl-1 anti-apoptotic function.
    MI-238 treatment (20 uM) induced apoptosis in 50.1 ± 1.1% of parental H1299 cells, but not Mcl-1 deficient H1299 cells, caused caspase 3 cleavage, effectively induced apoptosis in AML cells.
    MI-238 synergized with venetoclax to induce apoptosis in AML cells, and the combination of MI-238 and venetoclax potently inhibited the development of AML in murine model.

    物理化学性质&存储条件

    分子量 497.93
    分子式 C29H20ClNO5
    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

    N-(4-chloro-2-methylphenyl)-4-(naphthalen-2-yl)-2,4-dioxo-3-(3-oxo-1,3-dihydroisobenzofuran-1-yl)butanamide

    参考文献

    1. Tianming Zhao, et al. Mol Med. 2023 Jan 19;29(1):10.

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