CCG-1423

The Rho family of small GTPases play an important role in transduction of cell signaling events associated with several human cancers. CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription. It inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Galpha13 with an IC50 value of 1 µM. The site of inhibition in the pathway is not precisely defined but CCG-1423 appears to act on some aspect of the interaction of SRF with its transcriptional cofactor megakaryoblastic leukemia 1 (MKL1) at a point upstream of DNA binding. CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines at nanomolar to low micromolar concentrations.Formal Name: N-[2-[4(4-chlorophenyl)amino]-1-methyl-2-oxoethoxy]-3,5-bis(trifluoromethyl)-benzamide. CAS Number: 285986-88-1. Molecular Formula: C18H13ClF6N2O3. Formula Weight: 454.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.15 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 249 nm. SMILES: Clc1ccc(cc1)NC(=O)C(C)ONC(=O)c1cc(cc(c1)C(F)(F)F)C(F)(F)F. InChi Code: InChI=1S/C18H13ClF6N2O3/c1-9(15(28)26-14-4-2-13(19)3-5-14)30-27-16(29)10-6-11(17(20,21)22)8-12(7-10)18(23,24)25/h2-9H,1H3,(H,26,28)(H,27,29). InChi Key: DSMXVSGJIDFLKP-UHFFFAOYSA-N.