CCG-100602

Biochem/physiol Actions

CCG-100602 aids in preventing fibrosis around the temporomandibular joint (TMJ).

CCG-100602 is a CCG-1423 analog with significantly less cytotoxicity (0/14% WST-1 inhibition by 10/100 µM CCG-100602 vs. 44% by 10 µM CCG-1423) and similar efficacy against Rho/MKL1/SRF pathway-mediated transcription (by 78% with 100 µM CCG-100602 vs. 74% with 10 µM CCG-1423; IC50 = 9.8 µM/CCG-100602 vs. 1.5 µM/CCG-1423; by PC-3 SRE-luciferase assay), albeit at a reduced potency. CCG-100602 reduces the stiffening of spontaneously hypertensive rats (SHR) derived aortic VSMCs (1.12 µM) by inhibiting SRF/myocardin interaction and abrogates the increased aortic wall stiffness in SHR rats in vivo (7.5 mg/kg/d via s.c. osmotic pumps for 2 wks).