CCG-203971 MedChemExpress (MCE)

Product Name	CCG-203971
Synonyms	203971 CCG203971 CCG-203971 CCG 203971 N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide 3-Piperidinecarboxamide, N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-
CAS	1443437-74-8
EINECS
Chemical Formula	C23H21ClN2O3
Molecular Weight	408.88
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	CCG-203971 CCG-203971 MedChemExpress (MCE) HY-108361 1443437-74-8 98.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions CCG-203971 CCG-203971 MedChemExpress (MCE) HY-108361 1443437-74-8 98.0% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent. CCG-203971, a second-generation Ras homolog gene family, member A (RhoA)/myocardin-related transcription factor A (MRTF-A)/serum response factor (SRF) pathway inhibitor, represses both matrix-stiffness and transforming growth factor beta–mediated fibrogenesis as determined by protein and gene expression in a dose-dependent manner. CCG-203971 significantly represses TGF-β- induced MKL1 expression at 25 μM concentration[2]. Human dermal fibroblasts are plated onto 96-well plates and allowed to grow for 3 days in the presence of 30 μM CCG-203971 or DMSO vehicle. Viable cell density is assessed through enzymatic reduction of the water-soluble tetrazolium dye WST-1. Scleroderma dermal fibroblasts proliferate faster than normal cells, and this is inhibited by CCG-203971[3]. CCG-203971 is tested in a Bleomycin skin injury model. Bleomycin is administered in 50 μL of DMSO intraperitoneally. Preliminary studies show that Bleomycin administered in this manner is well tolerated at 100 mg/kg twice a day. Intradermal Bleomycin for 2 weeks along with the DMSO control (50 μL i.p.) results in marked dermal thickening (P[3]. Mice[3] Skin fibrosis is induced in C57BL/6 mice (female, 8 weeks old) by local intracutaneous injection of 100 μL of Bleomycin (1 mg/mL) in phosphate-buffered saline (PBS), every day for 2 weeks in a defined area (~1 cm2) on the upper back. Intracutaneous injection of 100 μL of PBS is used as a control. Three groups of mice with a total of 21 mice are used. One group receives injections of PBS and the other two are challenged with Bleomycin. Twice-a-day intraperitoneal administration of CCG-203971 (100 mg/kg in 50 μL of DMSO) is initiated together with the first challenge of Bleomycin and continues for 2 weeks. DMSO is used as the vehicle control. The three groups of animals are: (1) PBS/DMSO (2) Bleomycin/DMSO and (3) Bleomycin/CCG-203971. After treatment, animals are humanely killed by cervical dislocation, and tissue is collected[3]. Human dermal fibroblasts (2.0×104) are plated into a 96-well plate and grown overnight in DMEM containing 10% FBS. Media are removed and replaced with DMEM containing 2% FBS and 30 μM CCG-203971 or 0.1% DMSO control. After 72 hours WST-1 dye is added to each well, and after 60 minutes absorbance at 490 nm is read using a Wallac Victor2 plate reader[3]. RhoA/MRTF-A[1] Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Bell JL, et al. 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. [Content Brief] [2]. Johnson LA, et al. Novel Rho/MRTF/SRF inhibitors block matrix-stiffness and TGF-β-induced fibrogenesis in human colonic myofibroblasts. Inflamm Bowel Dis. 2014 Jan 20(1):154-65. [Content Brief] [3]. Haak AJ, et al. 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. [Content Brief]
Supplier Website	https://www.medchemexpress.com/CCG-203971.html
Last Update	2025-05-21 16:50:25

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