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).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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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