Rhosin Hcl is a specific Rho inhibitor; binds to WT RhoA with an affinity ~0.4 uM Kd; does not interfere with the binding of Cdc42 or Rac1.
Description :
Rhosin (G04) is a potent, specific RhoA subfamily Rho GTPases inhibitor that specifically binds to RhoA to inhibit GEF reaction of RhoA with Kd of 0.4 uM, does not interact with Cdc42 or Rac1, nor the LARG; specifically inhibits GEF activation of RhoA in vitro and in cells and can potently suppress breast cancer cell proliferation and invasion and induce neurite outgrowth in PC12 cells; strongly inhibits RhoA-GTP formation in NIH 3T3 cells (EC50=10-30 uM), reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres (EC50=30-50 uM); suppresses invasion of mammary epithelial cells, induces neurite outgrowth of PC12 cells in synergy with NGF.