CCG-203971 is a small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.
CCG-203971, a novel inhibitor of Rho-mediated gene transcription. CCG-203971 is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally[3]. CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM[4]. CCG-203971 has a significant reduction of melanoma metastasis and bleomycin- induced fibrosis[5]. CCG-203971, is also a novel small-molecule inhibitor of MRTF/SRF-regulated transcription, inhibits expression of connective tissue growth factor (CTGF), α-smooth muscle actin (α-SMA), and collagen 1 (COL1A2) in both SSc fibroblasts and in lysophosphatidic acid (LPA)-and transforming growth factor β (TGFβ)-stimulated fibroblasts. In vivo treatment with CCG-203971 also prevented bleomycin-induced skin thickening and collagen deposition[6].
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