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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-Compound II757
Compound II757

Chemical Structure : Compound II757

CAS No.:

Compound II757 (II757)

货号: PC-72716Not For Human Use, Lab Use Only.

Compound II757 (II757) is a potent, cell-active pan-PRMT inhibitor with IC50 of 5-555 nM for eight PRMTs, with the highest inhibition for PRMT4 (IC50=5 nM).

规格 价格 库存 数量
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Compound II757 (II757) is a potent, cell-active pan-PRMT inhibitor with IC50 of 5-555 nM for eight PRMTs, with the highest inhibition for PRMT4 (IC50=5 nM).
    II757 competitively binds at the SAM binding site of PRMT1, inhibits PRMT1 with an IC50 of 16 nM.
    II757 demonstrated modest inhibition to PRMT3 and PRMT7 (IC50=555 nM).
    II757 (0-100 uM) reduced histone H4 Arg3 asymmetric dimethylation (H4R3me2a) level in HEK293 cells
    II757 displays selectivity over a panel of other methyltransferases (SAHH, NTMT1, SETD7, G9a, NNMT, TbPRMT7 etc.).

    物理化学性质&存储条件

    分子量 537.437
    分子式 C20H25BrN8O3S
    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

    1-(3-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)propyl)-3-(3-bromophenyl)guanidine

    参考文献

    1. Iredia D Iyamu, et al. Biomolecules. 2021 Jun 8;11(6):854.

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