| Description |
A cell-permeable carbazolylpyrimidine compound that inhibits Rac GEF interaction (by 45% of Vav2 interaction at 4 µM and by 35% of Tiam1 DH/PH domain interaction at 50 µM) by directly targeting Rac GEF binding domain and effectively reduces cellular Rac1-GTP (IC 50 = 1.1 and 3 µM, respectively, in MDA-MB-435 and MDA-MB-231 cells) and Rac3-GTP (IC 50 <1 µM in MDA-MB-435 cells) as well as PAK Thr423 phosphorylation (by 55% and 84%, respectively, at 2 and 4 µM in MDA-MB-435 cells), suppressing MDA-MB-435 Cdc42-GTP level only at higher concentrations (by 5%, 18% and 75%, respectively, at 4, 5, and 10 µM) and enhancing, instead of downregulating, RhoA-GTP level, presumably due to a cellular compensatory mechanism in response to Rac inhibition
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