ZINC69391 是 Rac1 的选择性抑制剂，具有抗增殖和抗转移作用。 ZINC69391 干扰 Rac1 与 Dock180 的相互作用，降低 Rac1-GTP 水平并诱导细胞凋亡。

ZINC69391 is a selective inhibitor of Rac1 with antiproliferative and antimetastatic effects. ZINC69391 interferes with the interaction of Rac1 with Dock180, reduces Rac1-GTP levels and induces apoptosis.

In U-87 MG and LN229 cells, ZINC69391 (0-125 μM) reduces cell proliferation of human glioma cells. ZINC69391 (50-100 μM) triggers cell cycle arrest[1]. ZINC69391 inhibits the growth of U937, HL-60, KG1A, and Jurkat cells (IC50s = 41-54 μM). In HL-60, U937, and KG1A cell lines, ZINC69391 (50 μM) triggers an increase in apoptotic cells. In LN229 cells, ZINC69391 (50 and 100 μM) augments the enzymatic activity of caspase 3 and increases the percentage of cells in the sub-G0/G1 phase in a concentration-dependent manner[3].

In specific pathogen-free female BALB/c inbred mice (bearing F3II cells), ZINC69391 (25 mg/kg; i.p) impairs metastatic lung colonization and reduces by about 60% the formation of total metastatic lung colonies[2].

303094-67-9

C14H14F3N5

309.29

ZINC-69391;N'-(4,6-dimethylpyrimidin-2-yl)-N-[2-(trifluoromethyl)phenyl]guanidine

DMSO:20 mg/mL (64.66 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years