BI8622

Research use only, not for human use.

BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM.

BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b); abolishes ubiquitination of MCL1 induced by ectopically expressed HUWE1 in HeLa cells with IC50 of 6.8 uM, suppresses colony formation of Ls174T cells with IC50 of 8.4 uM; inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells; stabilizes MYC-associated protein MIZ1.

BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC50 value of 6.8 μM in HeLa cells.BI8622 suppresses colony formation of Ls174T cells with estimated IC50 value of 8.4 μM.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.BI8622 (0-50 μM; 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells. Cell Cycle Analysis 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 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.

——

BI-8622 | BI 8622

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

E3 Ubiquitin Ligase

——

——

1875036-74-0

426.524

C25H26N6O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (293.08 mM)

O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4

N-(4-(aminomethyl)phenyl)-6-(4-cyano-4-phenylpiperidin-1-yl)-5-methylpyrimidine-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years