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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-SKLB-03220
SKLB-03220

Chemical Structure : SKLB-03220

CAS No.: 2852050-29-2

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SKLB-03220 (SKLB03220)

货号: PC-49699Not For Human Use, Lab Use Only.

SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).

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

    生物&药学活性

    SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).
    SKLB-03220 binds the same location as the EPZ-6438, and forms a covalent bond with Cys663.
    SKLB-03220 (10 nM) showed good inhibitory activity against EZH2 mutants (EZH2 A677G, EZH2 Y641N, and EZH2 Y641F).
    SKLB-03220 does not exhibit inhibitory activity against other HMTases at 10 uM (G9a, SUV39H1, SETD8, SMYD2, PRMT1, PRMT5, and PRMT7), as well as a panel of 224 kinases by Eurofins Kinase Profiler.
    SKLB-03220 exhibited more potent proliferation inhibitory activity than reference compounds GSK126 and EPZ-6438, especially in human ovarian cancer cell lines.
    SKLB-03220 inhibited proliferation of ovarian cancer cell lines PA-1 and A2780 with IC50 of 10.1 and 11.2 uM, respectively, induced ovarian cancer cell apoptosis in a dose-dependent manner, inhibited the expression of H3K27me3 in ovarian cancer cells.
    SKLB-03220 (150 mg/kg, oral, twice daily) reduced the tumor growth in PA-1 tumor xenograft model in BALB/c nude mice, exhibited greater tumor growth inhibition (TGI) than EPZ-6438 (150 mg/kg) group.

    物理化学性质&存储条件

    分子量 556.71
    分子式 C33H40N4O4
    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

    5'-Acrylamido-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2',4-dimethyl-[1,1'-biphenyl]-3-carboxamide

    参考文献

    1. Qiangsheng Zhang, et al. J Med Chem. 2023 Jan 24. doi: 10.1021/acs.jmedchem.2c01370.

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