ZINC69391

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Chemical Structure| 303094-67-9 同义名 : -
CAS号 : 303094-67-9
货号 : A1549539
分子式 : C14H14F3N5
纯度 : 99%+
分子量 : 309.28
MDL号 : -
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(80.83 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ZINC69391 is a specific Rac1 inhibitor that interferes with Rac1-GEF interactions by shielding the Trp56 residue on the Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis and displays anti-proliferative and anti-metastatic effects[1][2][3].ZINC69391 inhibits the growth of U937, HL-60, KG1A and Jurkat cells with IC50 ranging from 41 to 54 μM[1]ZINC69391 at 50-100 μM for 24 hours enhances the enzymatic activity of caspase 3 in a concentration-dependent manner. Action of ZINC69391 at a concentration of 50 μM for 24 hours triggers apoptosis in human acute leukaemia cells[1].Cell proliferation of human glioma cells was reduced by ZINC69391 at a concentration range of 0-125 μM for 72 hours. Acting with ZINC69391 at concentrations of 50-100 μM for 48 hours triggers cell cycle arrest [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.23mL

0.65mL

0.32mL

16.17mL

3.23mL

1.62mL

32.33mL

6.47mL

3.23mL
参考文献

[1]Cabrera M, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017;8(58):98509‐98523. Published 2017 Oct 4.

[2]Cardama GA, et al. Proapoptotic and antiinvasive activity of Rac1 small molecule inhibitors on malignant glioma cells. Onco Targets Ther. 2014;7:2021‐2033. Published 2014 Oct 30.

[3]Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840‐851.