Biological Activity
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
| M. Wt | 408.88 |
| Formula | C23H21ClN2O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1443437-74-8 |
| PubChem ID | 71681561 |
| InChI Key | HERLZBNILRVHQN-UHFFFAOYSA-N |
| Smiles | O=C(N2CCCC(C(NC3=CC=C(Cl)C=C3)=O)C2)C1=CC=CC(C4=CC=CO4)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.44 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 408.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.45 mL | 12.23 mL | 24.46 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.89 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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References
References are publications that support the products' biological activity.
Michel et al (2014) Hope for disease-modifying treatment of systemic sclerosis/scleroderma. J.Pharmacol.Exp.Ther. 350 480 PMID: 25053235
Bell et al (2013) Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents. Bioorg.Med.Chem.Lett. 23 3826 PMID: 23707258
Haak et al (2014) 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. J.Pharmacol.Exp.Ther. 349 480 PMID: 24706986
Keywords: CCG 203971, supplier, CCG203971, antifibrotic, agent, inhibits, fibrosis, inhibitors, MRTF/SRF, gene, transcription, pathway, myocarin-related, transcription, factor, Systemic, sclerosis, connective, tissue, PC-3, cell, migration, Other, Transcription, Factors, Other, Transcription, Factors, Tocris Bioscience
