CCG-TH30

CCG-TH30 is a small molecule inhibitor of the Rho/MRTF/SRF (Serum Response Factor) signaling pathway, specifically targeting the transcriptional activity of Myocardin-Related Transcription Factors (MRTF-A and MRTF-B). Developed at the University of Michigan, CCG-TH30 was identified through high-throughput screening to block Rho-mediated activation of the SRF promoter. By inhibiting the formation or activity of the MRTF/SRF transcriptional complex, the compound suppresses the expression of genes involved in myofibroblast differentiation and epithelial-mesenchymal transition (EMT), such as alpha-smooth muscle actin (alpha-SMA). CCG-TH30 has demonstrated efficacy in preclinical models of systemic sclerosis (scleroderma) and cancer metastasis, particularly melanoma, by reducing fibrotic gene expression and inhibiting cellular migration. It serves as a chemical probe and a lead compound for the development of more potent analogs like CCG-203971.