In Vitro: H3B-6527 inhibits TAOK2, JNK2, and CSF1R with IC50s of 690 nM, >10000 nM, and >10000 nM, respectively. H3B-6527 (10-10000 nM; 72 hours) results in a GI50 value of 25 nM. H3B-6527 (10-10000 nM; 72 hours) leads cell death in HCC cell lines. H3B-6527 (0.1-1000 nM; 1 hour) decreases the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM. H3B-6527 (1-1000 nM; 24 hours) causes a robust increase in CYP7A1 transcripts.
In Vivo: H3B-6527 (10-300 mg/kg; orally; twice-daily; for 15 days) significantly inhibits tumor growth at the 300 and 100 mg/kg and does not inhibit tumor growth at 30 and 10 mg/kg.