BI8622

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

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme

IC50: 3.1 μM (HUWE1)[1]

BI8622 induces HUWE1 ectopically expresses to abolishe 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 values 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]. Cell Cycle Analysis[1] Cell Line: Ls174T cells Concentration: 0 μM, 5 μM,10 μM, 15 μM, 20 μM Incubation Time: 0-4 days Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0 μM, 10 μM, 20 μM Incubation Time: 16 hours Result: Retarded the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.

[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.