| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | AZA1 (Rac1/Cdc42-IN-1) (2-10 μM; 72 hours) blocks the proliferation of human prostate cancer cells 22Rv1 prostate cancer cells[1].AZA1 (2-10 μM; 24 hours) reduces phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells[1].AZA1 (10 μM; 24 hours) blocks Rac1 and Cdc42-dependent cell cycle events in 22Rv1 prostate cancer cells[1].AZA1 blocks Rac1 and Cdc42-dependent migration of 22Rv1, DU 145 and PC-3 prostate cancer cells[1].AZA1 affects cell motility and actin rearrangement in prostate cancer cells by suppressing Rac1 and Cdc42 activity via PAK1/2 phosphorylation[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | 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[1]. Animal Model: | ||||||||||||
| Name | AZA1 | ||||||||||||
| CAS | 1071098-42-4 | ||||||||||||
| Formula | C22H20N6 | ||||||||||||
| Molar Mass | 368.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Zins K, et al. A Rac1/Cdc42 GTPase-specific small molecule inhibitor suppresses growth of primary human prostate cancer xenografts and prolongs survival in mice. PLoS One. 2013;8(9):e74924. Published 2013 Sep 11. [2]. Suzuki O, et al. Sialylation and glycosylation modulate cell adhesion and invasion to extracellular matrix in human malignant lymphoma: Dependency on integrin and the Rho GTPase family. Int J Oncol. 2015;47(6):2091‐2099. |