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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-SMYD3 inhibitor 29
SMYD3 inhibitor 29

Chemical Structure : SMYD3 inhibitor 29

CAS No.: 2095160-79-3

SMYD3 inhibitor 29

货号: PC-72992Not For Human Use, Lab Use Only.

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 1.7 nM.

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

    生物&药学活性

    SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 11.7 nM.
    SMYD3 inhibitor 29 exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferative activity against HepG2 in 3D cell culture (GI50=1.04 uM).
    SMYD3 inhibitor 29 inhibits cellular MAP3K2 methylation.
    SMYD3 inhibitor 29 displayed high selectivity when tested against a panel of methyltransferases, namely, SMYD1-2, G9a, PRDM9, and PRMT5.

    物理化学性质&存储条件

    分子量 491.032
    分子式 C28H31ClN4O2
    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)-1-(4-(2-(4-(1-aminocyclopropyl)phenyl)-4-chloroquinoline-7-carbonyl)-2-methylpiperazin-1-yl)butan-1-one

    参考文献

    1. Huang C, et al. ACS Med Chem Lett. 2019 May 23;10(6):978-984.

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