CCG 203971

Biological Activity

CCG 203971 is an antifibrotic agent; inhibits fibrosis by targeting the MRTF/SRF gene transcription pathway. Selectively inhibits proliferation of SSc-derived dermal fibroblasts but not that of normal fibroblasts. Inhibits expression of CTGF, α-SMA, and COL1A2 in SSc fibroblasts as well as in LPA and in TGFβ-stimulated fibroblasts. Prevents bleomycin-induced skin thickening and collagen deposition in vivo. Also suppresses PC-3 cell migration in scratch wound assays (IC₅₀ = 4.2 μM).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
   Bell et al.
   Bioorg.Med.Chem.Lett., 2013;23:3826
2. Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury.
   Haak et al.
   J.Pharmacol.Exp.Ther., 2014;349:480
3. Hope for disease-modifying treatment of systemic sclerosis/scleroderma.
   Michel et al.
   J.Pharmacol.Exp.Ther., 2014;350:480

Product Datasheets