SIM1

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SIM1  纯度: 99.72%

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。

SIM1

SIM1 Chemical Structure

规格 价格 是否有货 数量
1 mg ￥10500 In-stock
5 mg ￥26500 In-stock
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50 mg   询价  

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SIM1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

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].

IC50 & Target

BRD2

1.1 nM (IC50)

BRD2

186 nM (Kd)

BRD3

 

BRD4

 

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 nM
Incubation Time: 30 hours
Result: Resulted in measurable cellular death after 6 hours.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1 µM
Incubation Time: 4 hours
Result: Degraded BET proteins.

分子量

1618.81

Formula

C79H98Cl2N14O13S3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献

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

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