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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-IHMT-337
IHMT-337

Chemical Structure : IHMT-337

CAS No.: 3018914-31-0

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IHMT-337 (IHMT337)

货号: PC-49674Not For Human Use, Lab Use Only.

IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.

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

    生物&药学活性

    IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.
    IHMT-337 demonstrates excellent selectivity for EZH2 over a wide range of methyltransferases including EZH1, covalently binds to EZH2 at Cys663 residue in SET domain.
    IHMT-337 showed comparable effects on H3K27me3 levels in different DLBCL cell lines in a dose-dependent manner, compared to EPZ6438 and GSK126.
    IHMT-337 robustly impaired EZH2-dependent DLBCL cell proliferation with similar GI50s.
    IHMT-337 (10 uM, 24 h) degrades EZH2 through CHIP E3 ligase-mediated proteasome pathway in both Pfeiffer and MDA-MB-231 cells.
    IHMT-337 inhibits breast cancer cell proliferation by degrading EZH2, a CDK4 transcription factor.
    IHMT-337 inhibits cell proliferation in different preclinical models in vitro and in vivo.

    物理化学性质&存储条件

    分子量 561.08
    分子式 C31H33ClN4O4
    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

    2'-acrylamido-4'-chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-[1,1'-biphenyl]-3-carboxamide

    参考文献

    1. Husheng Mei, et al. Signal Transduct Target Ther. 2023 Jan 16;8(1):18.

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