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Merck
CN

SML1421

Sigma-Aldrich

EPZ015666

≥98% (HPLC)

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别名:
(S)-N-(3-(3,4-二氢异喹啉-2 (1H)-基)-2-羟基丙基)-6-(氧杂坦-3-基氨基)嘧啶-4-甲酰胺, GSK3235025, YQ36286
经验公式(希尔记法):
C20H25N5O3
分子量:
383.44
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O[C@H](CN1CCC(C=CC=C2)=C2C1)CNC(C3=CC(NC4COC4)=NC=N3)=O

InChI

1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1

InChI key

ZKXZLIFRWWKZRY-KRWDZBQOSA-N

生化/生理作用

EPZ015666 (GSK3235025) 是一种蛋白质精氨酸甲基转移酶 PRMT5 抑制剂,在生物化学试验中 IC 50 值为 22 nM,在最高试验浓度 50 μM 时对20 种蛋白甲基转移酶的组合无抑制作用。相对于 SAM,抑制作用不具有竞争性。EPZ015666 在多种 体外 体内 套细胞淋巴瘤 (MCL) 模型中显示剂量依赖性抗肿瘤活性,处理 MCL 细胞系导致抑制 SmD3 甲基化和细胞死亡。

其他说明

化学探针门户网站已对 EPZ015666 进行了专家评审和推荐。欲了解更多信息,请访问化学探针门户网站上的 EPZ015666 探针摘要

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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