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UMB-32
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UMB-32图片
CAS NO:1635437-39-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
UMB-32 是一种有效的选择性 BRD4 抑制剂,结合 BRD4 的 Kd 为 550 nM,IC50 为 637 nM。 UMB-32 还显示出对 TAF1(一种含溴结构域的转录因子)的效力。
Cas No.1635437-39-6
化学名N-(1,1-dimethylethyl)-2-[4-(3,5-dimethyl-4-isoxazolyl)phenyl]-imidazo[1,2-a]pyrazin-3-amine
Canonical SMILESCC(C)(C)NC1=C(N=C2N1C=CN=C2)C3=CC=C(C4=C(C)ON=C4C)C=C3
分子式C21H23N5O
分子量361.4
溶解度≤20mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

UMB-32 is a potent, selective inhibitor of the BET bromodomain BRD4 [1]. The BET family (BRD2, BRD3, BRD4, and BRDT) functions as transcriptional coactivator proteins. BET bromodomains are also important mediators of cell cycle progression and facilitate developmental transitions such as spermiogenesis. Deregulation of BET bromodomain function has been observed in numerous malignancies. BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer [1].

In vitro: UMB-32 bound to BRD4 with a Kd value of 550 nM and 724 nM cellular potency in BRD4-dependent lines. UMB-32 showed potency against TAF1, a bromodomain-containing transcription factor. UMB-32 showed markedly increased potency for the BET proteins associated with a dramatic improvement in selectivity. UMB-32 potently bound to the TAF1 and TAF1L with the Kd values of 560nM and 1.3 μM, respectively [1].

Reference:
[1] McKeown M R, Shaw D L, Fu H, et al.  Biased multicomponent reactions to develop novel bromodomain inhibitors[J]. Journal of medicinal chemistry, 2014, 57(21): 9019-9027.