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CCG-203971

Cat. No. M8533

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CCG-203971 Structure
Size Price Availability Quantity
2mg USD 24  USD24 In stock
5mg USD 32  USD32 In stock
10mg USD 50  USD50 In stock
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Quality Control & Documentation
Biological Activity

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. In mouse studies, CCG-203971 inhibited invasion of PC-3 prostate cancer cells and was well tolerated up to doses of 100 mg/kg IP over 5 days.

The Rho/MRTF/SRF pathway has also been shown to be involved in multiple types of solid organ fibrosis. CCG-203971 repressed both matrix-stiffness and TGF-β-mediated fibrogenesis in human colonic myofibroblasts and showed antifibrotic activity in a murine model of skin injury and in pulmonary fibrosis lung fibroblasts.

Chemical Information
Molecular Weight 408.88
Formula C23H21ClN2O3
CAS Number 1443437-74-8
Solubility (25°C) DMSO ≥ 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Erika M Lisabeth, et al. Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Antifibrotic and Antimetastatic Compounds

[2] Zengdun Shi, et al. Myocardin and myocardin-related transcription factor-A synergistically mediate actin cytoskeletal-dependent inhibition of liver fibrogenesis

[3] Cynthia Yu-Wai-Man, et al. Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis

[4] Kim M Hutchings, et al. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma

[5] Bunta Watanabe, et al. Stereospecific Inhibitory Effects of CCG-1423 on the Cellular Events Mediated by Myocardin-Related Transcription Factor A

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Keywords: CCG-203971 supplier, Ras, inhibitors, activators

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