BI8622 是一种泛素连接酶 HUWE1 特异性拮抗剂，IC50 为 3.1 μM。
货号:ajcx39320
CAS:1875036-74-0
分子式:C25H26N6O
分子量：426.51
溶解度:DMSO : 125 mg/mL (293.08 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM[1].

BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC50 value of 6.8 μM in HeLa cells[1].BI8622 suppresses colony formation of Ls174T cells with estimated IC50 value of 8.4 μM[1].BI8622 (10 μM; 1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1[1].BI8622 (0-50 μM; 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells[1].BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells[1].

[1]. Peter S, et al. Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase. EMBO Mol Med. 2014 Dec;6(12):1525-41.