CCG-203971

Catalog No.S8469

For research use only.

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.

CCG-203971 Chemical Structure

CAS No. 1443437-74-8

Selleck's CCG-203971 has been cited by 2 Publications

Purity & Quality Control

Choose Selective Rho Inhibitors

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
Rho [1] 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 (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[2]

  • Animal Models: C57BL/6 mice
  • Dosages: 100 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 408.88
Formula

C23H21ClN2O3
 

CAS No. 1443437-74-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CN(C1)C(=O)C2=CC=CC(=C2)C3=CC=CO3)C(=O)NC4=CC=C(C=C4)Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

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.

Handling Instructions

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