ZINC69391 是一种特异的 Rac1 抑制剂，通过在 Rac1 表面掩蔽 Trp56 残基来干扰 Rac1-GEF 的相互作用。ZINC69391 干扰 Rac1 与 Dock180 的相互作用，降低 Rac1-GTP水平。ZINC69391 诱导细胞凋亡，具有抗增殖和抗转移作用。
| Cas No. | 303094-67-9 |
| 分子式 | C14H14F3N5 |
| 分子量 | 309.29 |
| 溶解度 | DMSO : 25 mg/mL (80.83 mM; ultrasonic and warming and heat to 60°C) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | ZINC69391, a specificRac1inhibitor, 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[1][2][3]. ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM[1].
ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner[1].
ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells[2].
ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest[2].
ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells[1]. Cell Proliferation Assay[2] | Cell Line: | U-87 MG, LN229 cells | | Concentration: | 0-125μM | | Incubation Time: | 72 hours | | Result: | Reduced cell proliferation in a concentration-dependent manner. |
Cell Cycle Analysis[2] | Cell 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 Analysis[1] | Cell Line: | HL-60, U937 and KG1A cell lines | | Concentration: | 50 μM | | Incubation Time: | 24 hours | | Result: | Led to a significant increase in apoptotic cells. |
ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3]. | Animal Model: | Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)[3] | | 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. |
|
m.cnreagent.com