MS645 ( MS-645;MS 645 )

产品货号. M17059 CAS No.

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

MS645
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ).
产品描述

MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2; shows comparable potency to the tandem BD1-BD2 of BRD2 and BRD3 as to that of BRD4; inhibits the transcription of BRD4 target gene IL-6 in MDA-MB-231 cells with 70% inhibition at 20 nM, much higher than 20-30% inhibition by JQ1 and MS417; potently inhibits cell growth of a panel TNBC with IC50 of 4-20 nM, blocks BRD4 binding to transcription enhancer/mediator proteins MED1 and YY1 with potency superior to monovalent BET inhibitors JQ1.
同义词

MS-645;MS 645
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

Bromodomain
研究领域

——
适应症

——

CAS Number

--
分子量

938.05
分子式

C48H54Cl2N10O2S2
纯度

>98% (HPLC)
溶解度

——
SMILES

——
化学全称

(S)-N,N'-(decane-1,10-diyl)bis(2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f] [1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)

1. Ren C, et al. Proc Natl Acad Sci U S A. 2018 Jul 16. pii: 201720000.

计算器

产品手册

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