Home Cell Cycle Rho inhibitor CCG-203971 For research use only.

CCG-203971

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

CCG-203971 Chemical Structure

CAS No. 1443437-74-8

Purity & Quality Control

CCG-203971 Related Products

Signaling Pathway

Rho Signaling Pathways

Rho Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 408.88 Formula

C23H21ClN2O3
 
CAS No. 1443437-74-8 SDF Download CCG-203971 SDF
Smiles C1CC(CN(C1)C(=O)C2=CC=CC(=C2)C3=CC=CO3)C(=O)NC4=CC=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (198.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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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