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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EPZ015666
EPZ015666

Chemical Structure : EPZ015666

CAS No.: 1616391-65-1

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EPZ015666 (EPZ-015666;GSK3235025)

货号: PC-43165Not For Human Use, Lab Use Only.

EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM, displays broad selectivity against a panel of other histone methyltransferases.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2480 In stock
50 mg ￥3980 In stock
100 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

EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM, displays broad selectivity against a panel of other histone methyltransferases.
EPZ015666 (GSK3235025) inhibits SmD3 methylation and causes cell death in MCL cell lines (IC50=61-904 nM).
EPZ015666 (GSK3235025) demonstrates potent concentration-dependent antiproliferative effects against Z-138 and Maver-1 cells with IC50 of 96 and 450 nM, respectively.
EPZ015666 (GSK3235025) exhibits antitumor activity in multiple MCL xenograft models.

物理化学性质&存储条件

分子量 383.4442
分子式 C20H25N5O3
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

DMSO: 10 mM (3.8 mg/mL)
Chemical Name/SMILES

4-Pyrimidinecarboxamide, N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-

参考文献

1. Chan-Penebre E, et al. Nat Chem Biol. 2015 Jun;11(6):432-7.

2. Kryukov GV, et al. Science. 2016 Mar 11;351(6278):1214-8.

3. Chan-Penebre E, et al. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6.

4. Gullà A, et al. Leukemia. 2018 Apr;32(4):996-1002.

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