Cat. No. 5277
Chemical Name: N-(4-Chlorophenyl)-1-[3-(2-furanyl)
Biological ActivityAntifibrotic agent; inhibits fibrosis by targeting the MRTF/SRF gene transcription pathway. Selectively inhibits proliferation of SSc-derived dermal fibroblasts but not that of normal fibroblasts. Inhibits expression of CTGF, α-SMA, and COL1A2 in SSc fibroblasts as well as in LPA and in TGFβ-stimulated fibroblasts. Prevents bleomycin-induced skin thickening and collagen deposition in vivo. Also suppresses PC-3 cell migration in scratch wound assays (IC50 = 4.2 μM).
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Haak et al (2014) Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury. J.Pharmacol.Exp.Ther. 349 480. PMID: 24706986.
Michel et al (2014) Hope for disease-modifying treatment of systemic sclerosis/scleroderma. J.Pharmacol.Exp.Ther. 350 480. PMID: 25053235.
Bell et al (2013) Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg.Med.Chem.Lett. 23 3826. PMID: 23707258.
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Keywords: CCG 203971, supplier, CCG203971, antifibrotic, agent, inhibits, fibrosis, inhibitors, MRTF/SRF, gene, transcription, pathway, myocarin-related, transcription, factor, Systemic, sclerosis, connective, tissue, PC-3, cell, migration, Tocris Bioscience, Other Transcription Factor products
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