Potent TGF-βRI (ALK-5) inhibitor (IC50 = 34 nM). Inhibits TGF-β transcriptional activation. Inhibits TGF-β-induced proliferation of lung epithelial cells and SMAD phosphorylation. Inhibits TGF-β-induced epithelial-to-mesenchymal transition (EMT). Also inhibitor of p38 MAPK. Likely active metabolite of A 83-01 (Cat. No. 2939).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 286.33. 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||3.49 mL||17.46 mL||34.92 mL|
|5 mM||0.7 mL||3.49 mL||6.98 mL|
|10 mM||0.35 mL||1.75 mL||3.49 mL|
|50 mM||0.07 mL||0.35 mL||0.7 mL|
References are publications that support the biological activity of the product.
Tojo et al (2005) The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer Sci. 96 791 PMID: 16271073
Sawyer et al (2003) Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain. J.Med.Chem. 46 3953 PMID: 12954047
If you know of a relevant reference for A 77-01, please let us know.
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Keywords: A 77-01, A 77-01 supplier, A77-01, A7701, transforming, growth, factor, receptor, TGF, B, beta, β, type, I, kinase, inhibitors, inhibits, potent, p38, MAPK, A, 83-01, A83-01, TGF-beta, Receptors, BMP, and, Other, Activin, 6712, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.