iHCK-37 (ASN05260065) is a potent and selective Hck inhibitor with Ki of 0.22 uM.
iHCK-37 displays high selectivity against a panel of kinases including other Src family members (Blk, Fgr, Fyn, cSRC, Lck, Lyn, Syk, and Yes), tyrosine kinases (Abl and Abl-T315I), as well as some kinases important for HIV1 (CDK9, FAK, Itk, JAK3, Ron).
iHCK-37 has anti-neoplastic activity in leukemia cells without altering apoptosis and survival rate of normal cells.
iHCK-37 demonstrates additive effects against leukemia cells combined with 5-Azacytidine or Cytarabine, reduces the activation of oncogenic pathways, MAPK/ERK and PI3K/AKT, leading to reduction of ERK and AKT phosphorylation, and increases BAX and decreased BCL-XL protein expression.
iHCK-37 exhibits antiproliferative activity profile against the human leukemia cell line KU-812 (IC50=66.5 uM).
iHCK-37 also blocks HIV-1 replication with EC50 of 12.9 uM.