SIM1 - ≥99% , CAS No.2719051-84-8

CAS: 2719051-84-8 Cat. No.: S649816 分子式: C₇₉H₉₈Cl₂N₁₄O₁₃S₃ 分子量: 1618.81

グレード＆純度 ≥99%

Storage

Protected from light,Store at -20°C,Argon charged

Shipped In

Ice chest + Ice pads

Application

PROTAC

概要

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

仕様

仕様と純度

≥99%

生化学的・生理学的メカニズム

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.

保管条件

Protected from light,Store at -20°C,Argon charged

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

純度

≥99%

名前と識別子

分子量

1618.81

化学的性質と物理的性質

• 溶解度: DMSO : 100 mg/mL (61.77 mM; Need ultrasonic)