BI8622

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC₅₀ of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM^{[1][2][3][4][5]}. IC50 & Target:IC50: 3.1 μM (HUWE1)^[1] In Vitro:BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC₅₀ value of 6.8 μM in HeLa cells^[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].
BI8622 (1 nM-10 μM) inhibits HUWE1 with an IC₅₀ of 3.1 μM^[1].
BI8622 (5-25 μM) suppresses colony formation of Ls174T cells^[1].
BI8622 results in higher TTBK2 levels in RPE1 cells^[5]. In Vivo:BI8622 (5 mg/kg, i.p., 6 h before cisplasin then once daily) significantly ameliorates cisplatin-induced renal dysfunction in cisplatin-induced AKI mouse model^[4].