常用名 SIM1

英文名 SIM1

CAS号 2719051-84-8

分子量 1618.81

密度 1.39±0.1 g/cm3(Predicted)

沸点 N/A

分子式 C79H98Cl2N14O13S3

熔点 N/A

 SIM1用途

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation ( IC 50 =1.1 nM; Kd =186 nM). SIM1 shows sustained anti-cancer activity In Vitro SIM1 (1 nM; 30 hours; MV4-11 cells) results in measurable cellular death after 6 hours. SIM1 (1 µM; 4 hours; HEK293 cells) degrades BET proteins. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MV4-11 cells Concentration: 1 nM Incubation Time: 30 hours Result: Resulted in measurable cellular death after 6 hours. Western Blot AnalysisCell Line: HEK293 cells Concentration: 1 µM Incubation Time: 4 hours Result: Degraded BET proteins. Form:Solid IC50& Target:BRD2 1.1 nM (IC 50 ) BRD2 186 nM (Kd) BRD3 BRD4

 SIM1名称

英文名 SIM1

密度 1.39±0.1 g/cm3(Predicted)

分子式 C79H98Cl2N14O13S3

分子量 1618.81

储存条件 避光,-20°C储存,充氩

水溶解性 DMSO : 100 mg/mL (61.77 mM; Need ultrasonic)

产地：西安

用途：科研

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研！

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