CCG-203971

Catalog No.S8469 Batch:S846901

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Technical Data

Formula

C23H21ClN2O3
 
Molecular Weight 408.88 CAS No. 1443437-74-8
Solubility (25°C)* In vitro DMSO 81 mg/mL (198.1 mM)
Ethanol 4 mg/mL (9.78 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[2]
  • Animal Models

    C57BL/6 mice

  • Dosages

    100 mg/kg

  • Administration

    i.p.

Selleck's CCG-203971 has been cited by 3 publications

Persistent Hypoxia with Intermittent Aggravation Causes Imbalance in Smad3/Myocardin-Related Transcription Factor Signaling with Consequent Endothelial Senescence and Pulmonary Arterial Remodeling [ Biomedicines, 2023, 11(9)2351] PubMed: 37760802
MKL1 mediates TGF-β-induced CTGF transcription to promote renal fibrosis. [ J Cell Physiol, 2020, 235(5):4790-4803] PubMed: 31637729
Targeting effector pathways in RAC1P29S-driven malignant melanoma. [ Small GTPases, 2020, 10.1080/21541248] PubMed: 32043900

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.