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Description: CCG-203971 is a novel, 2nd generation small-molecule inhibitor of the Rho/MRTF/SRF RhoA/myocardin-related transcription factor A (MRTF-A) pathway with an IC50 value of 0.64 uM for SRE. CCG-203971 inhibits expression of connective tissue growth factor (CTGF), alpha-smooth muscle actin (alpha-SMA), and collagen 1 (COL1A2) in both SSc fibroblasts and in lysophosphatidic acid (LPA)-and transforming growth factor beta (TGFbeta)-stimulated fibroblasts. CCG-203971 significantly represses TGF-beta- induced MKL1 expression at 25 uM concentration.
References: J Pharmacol Exp Ther. 2014 Jun; 349(3):480-6; Bioorg Med Chem Lett. 2017 Apr 15; 27(8):1744-1749.
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