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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-MS645
MS645

Chemical Structure : MS645

CAS No.: 2250091-96-2

MS645 (MS-645;MS 645)

货号: PC-35423Not For Human Use, Lab Use Only.

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.

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3280 In stock
50 mg ¥5480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
MS645 shows comparable potency to the tandem BD1-BD2 of BRD2 and BRD3 as to that of BRD4.
MS645 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.
MS645 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.

物理化学性质&存储条件

分子量 938.048
分子式 C48H54Cl2N10O2S2
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

(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)

参考文献

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

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