Description
CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971 . CCG-232601 inhibits MRTF-dependent transcription in HEK293T cells (IC
50 = 0.55 μM in a luciferase reporter assay). It also reduces expression of α-smooth muscle actin (α-SMA) in TGF-β-stimulated human dermal fibroblasts to 31% of control when used at a concentration of 10 μM. CCG-232601 (50 mg/kg) inhibits increases in dermal thickness and hydroxyproline content in a mouse model of dermal fibrosis induced by bleomycin .
