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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).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 408.88. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.89 mL||24.46 mL||48.91 mL|
|2.5 mM||0.98 mL||4.89 mL||9.78 mL|
|5 mM||0.49 mL||2.45 mL||4.89 mL|
|25 mM||0.1 mL||0.49 mL||0.98 mL|
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for CCG 203971, please let us know.
Keywords: CCG 203971, CCG 203971 supplier, CCG203971, antifibrotic, agent, inhibits, fibrosis, inhibitors, MRTF/SRF, gene, transcription, pathway, myocarin-related, factor, Systemic, sclerosis, connective, tissue, PC-3, cell, migration, Other, Transcription, Factors, 5277, Tocris Bioscience
3 Citations for CCG 203971
Citations are publications that use Tocris products. Selected citations for CCG 203971 include:
Lionarons et al (2019) RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance. Cancer Cell 36 68 PMID: 31257073
Zhu et al (2017) Similar regulatory mechanisms of caveolins and cavins by myocardin family coactivators in arterial and bladder smooth muscle. PLoS One 12 e0176759 PMID: 28542204
Osmanagic-Myers et al (2018) Endothelial progerin expression causes cardiovascular pathology through an impaired mechanoresponse. J Clin Invest PMID: 30422822
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Literature in this Area
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