BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC 50 of 0.9 μM
In Vitro
BI8626 induces HUWE1 ectopically expresses to abolishe ubiquitination of MCL1 in HeLa cells. ?\nBI8626 suppresses colony formation of Ls174T cells with estimated IC 50 value of 0.7 μM, and BI8622 (1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1. ?\nBI8626 (0-50 μM; 0-6 hours) retards the degradation of MCL1 in response to UV irradiation to the same extent as depletion of HUWE1 in U2OS cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell 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 AnalysisCell Line: U2OS cells Concentration: 0 μM, 20 μM, 50 μM Incubation Time: 0 hour,1 hour,2 hours,4 hours,6 hours Result: Retarded the degradation of MCL1 in response to UV irradiation in HeLa cells by inhibiting HUWE1 in U2OS cells.