ZINC69391 is a specific Rac1 inhibitor that interferes with Rac1-GEF interactions by shielding the Trp56 residue on the Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis and displays anti-proliferative and anti-metastatic effects[1][2][3].ZINC69391 inhibits the growth of U937, HL-60, KG1A and Jurkat cells with IC50 ranging from 41 to 54 μM[1]ZINC69391 at 50-100 μM for 24 hours enhances the enzymatic activity of caspase 3 in a concentration-dependent manner. Action of ZINC69391 at a concentration of 50 μM for 24 hours triggers apoptosis in human acute leukaemia cells[1].Cell proliferation of human glioma cells was reduced by ZINC69391 at a concentration range of 0-125 μM for 72 hours. Acting with ZINC69391 at concentrations of 50-100 μM for 48 hours triggers cell cycle arrest [2].
ZINC69391 动物研究
Animal study
Intraperitoneal daily administration of ZINC69391 to animals at a dose of 25 mg/kg for 21 days impairs metastatic lung colonisation in a syngeneic animal model, with a significant reduction in total metastatic lung colony formation of approximately 60% [3].
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