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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AM-9934
AM-9934

Chemical Structure : AM-9934

CAS No.: 2691869-48-2

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AM-9934 (AM9934)

货号: PC-24610Not For Human Use, Lab Use Only.

AM-9934 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of12 nM for PRMT5 methyltransferase activity and 40 nM for PRMT5:MEP50 enzymatic affinity, selectively inhibits PRMT5 in MTAP-deleted cells.

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

    生物&药学活性

    AM-9934 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of12 nM for PRMT5 methyltransferase activity and 40 nM for PRMT5:MEP50 enzymatic affinity, selectively inhibits PRMT5 in MTAP-deleted cells.
    AM-9934 has Kd of 55 nM in the presence of MTA using microscale thermophoresis (MST), with much weaker to either the apo enzyme or the SIN-bound enzyme (>10 uM).
    AM-9934 is highly selective for MTA-bound PRMT5.
    AM-9934 is selective against a broad panel of arginine-, lysine-, and DNA-methyltransferases.
    AM-9934 shows enhanced potency in the MTAP-deleted line (IC50 of 9.2 nM) and only weakly reduced SDMA in parental HCT116 cells (IC50 of 143 nM).
    AM-9934 inhibits cell viability more potently against MTAP-deleted cells (IC50 of 0.16 µM vs. 4.1 µM in parental cells.
    AM-9934 suppresses SDMA levels in MTAP-deleted tumors.

    物理化学性质&存储条件

    分子量 416.45
    分子式 C22H23F3N4O
    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-amino-N-isobutyl-3-methyl-N-((5-(trifluoromethyl)pyridin-2-yl)methyl)quinoline-6-carboxamide

    参考文献

    1. Andersson J, et al. Proc Natl Acad Sci U S A. 2025 May 20;122(20):e2425052122.

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