BI8622

• CAT Number: I019181
• CAS Number: 1875036-74-0
• Molecular Formula: C25H26N6O
• Molecular Weight: 426.51
• Purity: ≥95%
• Synonyms: N-[4-(aminomethyl)phenyl]-6-(4-cyano-4-phenylpiperidin-1-yl)-5-methylpyrimidine-4-carboxamide
• InChI: InChI=1S/C25H26N6O/c1-18-22(24(32)30-21-9-7-19(15-26)8-10-21)28-17-29-23(18)31-13-11-25(16-27,12-14-31)20-5-3-2-4-6-20/h2-10,17H,11-15,26H2,1H3,(H,30,32)
• InChIKey: IJHAXMJRQQTBPL-UHFFFAOYSA-N
• SMILES: CC1=C(N=CN=C1N2CCC(CC2)(C#N)C3=CC=CC=C3)C(=O)NC4=CC=C(C=C4)CN

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].

Reference

[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.
 [Content Brief]