ZINC69391

ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis , and shows antiproliferative and antimetastatic effects .

In Vitro

ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC 50 s ranging from 41 to 54 μM. ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner. ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells. ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest. ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: U-87 MG, LN229 cells Concentration: 0-125μM Incubation Time: 72 hours Result: Reduced cell proliferation in a concentration-dependent manner. Cell Cycle AnalysisCell Line: LN229 cells Concentration: 50, 100 μM Incubation Time: 48 hours Result: Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner. Apoptosis AnalysisCell Line: HL-60, U937 and KG1A cell lines Concentration: 50 μM Incubation Time: 24 hours Result: Led to a significant increase in apoptotic cells.

In Vivo

ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)Dosage: 25 mg/kg body weight Administration: I.p; daily for 21 days Result: Significantly reduced by about 60% the formation of total metastatic lung colonies.