CCG-203971

For research use only.

Catalog No.S8469

2 publications

CCG-203971 Chemical Structure

Molecular Weight(MW): 408.88

CCG-203971 is a novel 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.

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Biological Activity

Description CCG-203971 is a novel 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.
Targets
SRE.L [1]
()
0.64 μM
In vitro

CCG-203971 inhibits expression of connective tissue growth factor (CTGF), α-smooth muscle actin (α-SMA), and collagen 1 (COL1A2) in both SSc fibroblasts and in lysophosphatidic acid (LPA)-and transforming growth factor β (TGFβ)-stimulated fibroblasts[2].

In vivo CCG-203971 exhibits promising anti-fibrotic activity both in vitro and in vivo in several animal models of disease, including intestinal fibrosis, pulmonary fibrosis and dermal fibrosis. The half-life of CCG-203971 in mouse liver microsomes (MLM) is only 1.6 min, indicating high susceptibility to oxidative metabolism[1]. In vivo treatment with CCG-203971 also preventes bleomycin-induced skin thickening and collagen deposition[2].

Protocol

Cell Research:

[2]

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  • Cell lines: Dermal fibroblasts
  • Concentrations: 30 μM
  • Incubation Time: 72 h
  • Method:

    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 was read.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: C57BL/6 mice
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (198.1 mM)
Ethanol 4 mg/mL (9.78 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 408.88
Formula

C23H21ClN2O3
 

CAS No. 1443437-74-8
Storage powder
in solvent
Synonyms N/A
Smiles ClC1=CC=C(NC(=O)C2CCCN(C2)C(=O)C3=CC(=CC=C3)C4=CC=CO4)C=C1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID