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1922098-69-8

1922098-69-8 structure
1922098-69-8 structure
  • Name: CCG-222740
  • Chemical Name: CCG-222740
  • CAS Number: 1922098-69-8
  • Molecular Formula: C23H19ClF2N2O3
  • Molecular Weight: 444.86
  • Catalog: Signaling Pathways GPCR/G Protein Ras
  • Create Date: 2019-12-07 13:54:54
  • Modify Date: 2024-01-08 11:07:14
  • CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].

Name CCG-222740
Description CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].
Related Catalog
Target

Rho/MRTF pathway[1]

In Vitro CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreased cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM[1]. CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts[2]. CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic[2]. Cell Cycle Analysis[1] Cell Line: Cancer associated fibroblasts (CAFs) Concentration: 10, 20 μM Incubation Time: 72 hours Result: Increased the protein levels of p27 and decreased cyclin D1.
In Vivo CCG-222740 (Oral gavage; 100 mg/kg daily for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice[1]. Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks[1] Dosage: 100 mg/kg Administration: Oral gavage; daily; for 7 days Result: Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
References

[1]. Leal AS, et al. The Rho/MRTF pathway inhibitor CCG-222740 reduces stellate cell activation and modulates immune cell populations in KrasG12D; Pdx1-Cre (KC) mice. Sci Rep. 2019 May 8;9(1):7072.

[2]. Yu-Wai-Man C, et al. Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis. Sci Rep. 2017 Mar 31;7(1):518.

Molecular Formula C23H19ClF2N2O3
Molecular Weight 444.86
Storage condition -20°C