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Submit ReviewCCG 203971 is an 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).
分子量 | 408.88 |
公式 | C23H21ClN2O3 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1443437-74-8 |
PubChem ID | 71681561 |
InChI Key | HERLZBNILRVHQN-UHFFFAOYSA-N |
Smiles | O=C(N2CCCC(C(NC3=CC=C(Cl)C=C3)=O)C2)C1=CC=CC(C4=CC=CO4)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 CCG 203971 的部分引用包括:
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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