Rac1-IN-1

Rac1-IN-1 is a potent Rac1 inhibitor with an IC₅₀ of 95 nM and a K_i of 6.8 μM. Rac1-IN-1 blocks the binding of Rac1 to downstream PAK1 by targeting the nucleotide-binding site of Rac1, thereby specifically inhibiting Rac1 activation without affecting Cdc42/RhoA. Rac1-IN-1 can be used for research on pancreatic cancer^[1]. In Vitro:Rac1-IN-1 (compound #1) (1-50 µM; 2 h) dose-dependently inhibits EGF (HY-P7109)-stimulated Rac1 activation in CD18/HPAF cells, with an EC₅₀ of 8.3 µM^[1].
Rac1-IN-1 (25 µM; 24-120 h) inhibits the proliferation of Capan1, CD18/HPAF, and AsPC-1 pancreatic cancer cells^[1].
Rac1-IN-1 (1-75 µM; 24-48 h) inhibits the migration and invasion of Capan1 and CD18/HPAF cells^[1].
Rac1-IN-1 (1.6-100 µM; 7 days) reduced the viability of AsPC-1, Capan1, and CD18/HPAF pancreatic cancer cells with EC₅₀ values of 19.1, 21.7, and 22.5 µM, respectively, without affecting HPNE normal pancreatic ductal cells^[1].
Rac1-IN-1 (25-50 μM; 7 days) reduces cell colony formation in Capan1 cells.
Rac1-IN-1 (0.001-100 µM; 1 h) dose-dependently blocks the binding of Rac1-GTP to the downstream effector protein PAK1, with an IC₅₀ of 95 nM^[1].
Rac1-IN-1 (0.1-1000 µM; 1 h) dose-dependently displaced the nucleotide mant-GDP bound to Rac1 in an in vitro fluorescence polarization assay, with a K_i of 6.8 μM^[1].
Rac1-IN-1 (50 µM; 2 h) selectively inhibits Rac1 activity, but not Cdc42 and RhoA, in CD18/HPAF cells^[1].