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SIM1
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。
SIM1图片
规格:98%
分子量:1618.81
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
SIM1 是一种有效的 von Hippel-Lindau (VHL)-based PROTAC,能够对所有BET 家族成员进行降解,并优先降解 BRD2 (IC50=1.1 nM; Kd=186 nM)。SIM1显示出持续的抗癌活性。
货号:ajcx36342
CAS:N/A
分子式:C79H98Cl2N14O13S3
分子量:1618.81
溶解度:N/A
纯度:98%
存储:Store at -20°C
库存:现货

Background:

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity[1].

SIM1 (1 nM; 30 hours; MV4-11 cells) results in measurable cellular death after 6 hours[1].SIM1 (1 µM; 4 hours; HEK293 cells) degrades BET proteins[1].SIM1 induces conformational changes upon binding to the BET protein to simultaneously engage with high avidity both its bromodomains in a cis intramolecular fashion. SIM1 engages BD1 and BD2 intramolecularly and forms a 1:1:1 ternary complex with VHL and BRD4[1].

[1]. Satomi Imaide, et al. Trivalent PROTACs enhance protein degradation through cooperativity and avidity. Biological and Medicinal Chemistry.