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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EZM2302
EZM2302

Chemical Structure : EZM2302

CAS No.: 1628830-21-6

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EZM2302 (GSK3359088, GSK 3359088, EZM 2302)

货号: PC-61030Not For Human Use, Lab Use Only.

EZM2302 (EZM 2302, GSK 3359088) is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM, with broad selectivity against other HMTases.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 99.5% (HPLC) Select Batch:

生物&药学活性

EZM2302 (EZM 2302, GSK 3359088) is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM, with broad selectivity against other HMTases.
EZM 2302 demonstrates in vitro anti-proliferative activity consistent with specific methyl mark inhibition with IC50 of <100 nM in 9/15 multiple myeloma cell lines, decreases methylation of PABP1 (IC50 =38 nM) and SmB (IC50=18 nM).
EZM 2302 displays dose-dependent inhibition of CARM1 substrate methylation in vivo, and induces growth inhibition of human multiple myeloma tumor xenografts in mice.

物理化学性质&存储条件

分子量 585.102
分子式 C29H37ClN6O5
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

100 mM in DMSO
Chemical Name/SMILES

methyl (R)-2-(2-(2-chloro-5-(2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate

参考文献

1. Drew AE, et al. Sci Rep. 2017 Dec 21;7(1):17993.

2. Greenblatt SM, et al. Cancer Cell. 2018 Jun 11;33(6):1111-1127.e5.

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