| Bioactivity | 1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo[1][2][3]. | ||||||||||||
| Invitro | 1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC50s of 4 µM and 21 µM, respectively[1].1A-116 (1, 10 µM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells[1].1A-116 (50, 100 µM; 12 h) blocks Rac1-P-Rex1 interaction[1].1A-116 (20 µM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner[2].1A-116 (10 µM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS))[2].1A-116 (20, 50 µM; 6 h) induces cells apoptosis and in a circadian-dependent manner[2].1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level[3]. Cell Proliferation Assay[1][2] Cell Line: | ||||||||||||
| Name | 1A-116 | ||||||||||||
| CAS | 1430208-73-3 | ||||||||||||
| Formula | C16H16F3N3 | ||||||||||||
| Molar Mass | 307.31 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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1A-116
CAS: 1430208-73-3 F: C16H16F3N3 W: 307.31
1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-
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