hck-in-1

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

PP487 is a dual tyrosine kinase PI(3)K inhibitor, exhibiting IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. It is applicable in cancer research [1].

iHCK-37 (ASN05260065) is a high-potency, selective inhibitor of Hck with a Ki value of 0.22 μM. It effectively inhibits HIV-1 viral replication with an EC50 value of 12.9 μM. Primarily employed in chronic myeloid leukemia (CML) research, iHCK-37 demonstrates promising potential for studying and understanding this disease.

BT424, a specific HCK inhibitor, modulates macrophage activation and autophagy in vitro, and mitigates inflammation and renal fibrosis in the UUO model [1].

KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2].