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BRD0639
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。
BRD0639图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍
BRD0639 是一类抑制 PRMT5-substrate adaptor interaction 的抑制剂。BRD0639 是一种 PRMT5 结合基序 (PBM) 竞争剂,可以支持 PBM 依赖的 PRMT5 活性的研究。
分子式C21H22ClN5O4S
分子量475.95
溶解度DMSO : 250 mg/mL (525.27 mM; Need ultrasonic)
储存条件Store at -20°C
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

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities[1].

BRD0639 is a first-in-class PBM-competitive small molecule that can support studies of PBM dependent PRMT5 activities and the development of novel PRMT5 inhibitors that selectively target these functions. BRD0639 can engage the cellular target and effectively outcompete binding between full-length PRMT5 and RIOK1 proteins with an IC50 of 7.5 uM and 16 uM in permeabilized and living cells, respectively. BRD0639 reduces SDMA in the same subset of proteins also affected by genetic perturbation of the PRMT5 binding motif (PBM) binding site[1].

[1]. McKinney DC, et al. Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction. J Med Chem. 2021;64(15):11148-11168.