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CCG-203971
CCG-203971
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货号：A415352
CCG-203971 is a small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.
CCG-203971 化学结构
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CCG-203971 纯度/质量文件 产品仅供科研
货号：A415352
标准纯度：
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CCG-203971 质控信息
CCG-203971 生物活性
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CCG-203971, a novel inhibitor of Rho-mediated gene transcription. CCG-203971 is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally[3] [4] [5] [6]
CCG-203971 参考文献
[1] Johnson LA, Rodansky ES, et al. Optimisation of Intestinal Fibrosis and Survival in the Mouse S. Typhimurium Model for Anti-fibrotic Drug Discovery and Preclinical Applications. J Crohns Colitis. 2016 Dec 16. pii: jjw210.
[2] Haak AJ, Appleton KM, et al. Pharmacological Inhibition of Myocardin-related Transcription Factor Pathway Blocks Lung Metastases of RhoC-Overexpressing Melanoma. Mol Cancer Ther. 2017 Jan;16(1):193-204.
[3] Hutchings KM, Lisabeth EM, Rajeswaran W, Wilson MW, Sorenson RJ, Campbell PL, Ruth JH, Amin A, Tsou PS, Leipprandt JR, Olson SR, Wen B, Zhao T, Sun D, Khanna D, Fox DA, Neubig RR, Larsen SD. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749
[4] Bell JL, Haak AJ, Wade SM, Kirchhoff PD, Neubig RR, Larsen SD. Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3826-32
[5] Lisabeth EM, Kahl D, Gopallawa I, Haynes SE, Misek SA, Campbell PL, Dexheimer TS, Khanna D, Fox DA, Jin X, Martin BR, Larsen SD, Neubig RR. Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Antifibrotic and Antimetastatic Compounds. ACS Pharmacol Transl Sci. 2019 Apr 12;2(2):92-100
[6] Haak AJ, Tsou PS, Amin MA, Ruth JH, Campbell P, Fox DA, Khanna D, Larsen SD, Neubig RR. 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. 2014 Jun;349(3):480-6
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CCG-203971 实验方案
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1mg
5mg
10mg
1 mM
5 mM
10 mM
2.45mL
0.49mL
0.24mL
12.23mL
2.45mL
1.22mL
24.46mL
4.89mL
2.45mL
CCG-203971 技术信息
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