AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
体外研究
AZA1 (Rac1/Cdc42-IN-1) (2-10 μM; 72 hours) blocks the proliferation of human prostate cancer cells 22Rv1 prostate cancer cells.
AZA1 (2-10 μM; 24 hours) reduces phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells.
AZA1 (10 μM; 24 hours) blocks Rac1 and Cdc42-dependent cell cycle events in 22Rv1 prostate cancer cells.
AZA1 blocks Rac1 and Cdc42-dependent migration of 22Rv1, DU 145 and PC-3 prostate cancer cells.
AZA1 affects cell motility and actin rearrangement in prostate cancer cells by suppressing Rac1 and Cdc42 activity via PAK1/2 phosphorylation.
Cell Proliferation Assay
Cell Line:
22Rv1 prostate cancer cells
Concentration:
2, 5, 10 μM
Incubation Time:
72 hours
Result:
Suppressed 22Rv1 prostate cancer cell proliferation in both unstimulated and EGF-stimulated cancer cells in a dose-dependent manner.
Western Blot Analysis
Cell Line:
22Rv1 prostate cancer cells (EGF-stimulated)
Concentration:
2, 5, 10 μM
Incubation Time:
24 hours
Result:
Reduced phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells.
体内研究
AZA1 (Rac1/Cdc42-IN-1) (100 μg; i.p.; daily for 2 weeks) is potent in suppressing human 22Rv1 xenograft growth in mice and improving survival.