Description
CCG1423 is an inhibitor of Rho signaling that inhibits serum response factor (SRF); it displays anti-metastatic, anti-diabetic, and anti-fibrotic activities. CCG1423 binds myocardin-related transcription factor A (MRTF-A), preventing its accumulation and potentially inhibiting the epithelial-to-mesenchymal transition (EMT). CCG1423 also inhibits invasiveness of prostate cancer cells. In animal models of diabetes pathogenesis, this compound improves glucose uptake and tolerance.
References
Hayashi K, Watanabe B, Nakagawa Y, et al. RPEL proteins are the molecular targets for CCG-1423, an inhibitor of Rho signaling. PLoS One. 2014 Feb 18;9(2):e89016. PMID: 24558465.
Bell JL, Haak AJ, Wade SM, et al. Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3826-32. PMID: 23707258.
Jin W, Goldfine AB, Boes T, et al. Increased SRF transcriptional activity in human and mouse skeletal muscle is a signature of insulin resistance. J Clin Invest. 2011 Mar;121(3):918-29. PMID: 21393865.