货号 | 5277/50 |
别名 | N-(4-Chlorophenyl)-1-[3-(2-furanyl) |
供应商 | Tocris |
生物活性 | Antifibrotic 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). |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 408.88 |
分子式 | C23H21ClN2O3 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
参考文献 | Haaket 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. Michelet al (2014) Hope for disease-modifying treatment of systemic sclerosis/scleroderma. J.Pharmacol.Exp.Ther. 350 480. PMID: 25053235. Bellet 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. |