SIM1,2719051-84-8

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SIM1

CAS No. : 2719051-84-8

MCE 国际站：SIM1

产品活性：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。

研究领域：PROTAC  |  Epigenetics

作用靶点：PROTACs  |  Epigenetic Reader Domain

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.

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