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Submit ReviewA 77-01
Description: Potent inhibitor of TGF-βRI
Chemical Name: 4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline
Purity: ≥98% (HPLC)
Biological Activity for A 77-01
A 77-01 is a 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).
Compound Libraries for A 77-01
A 77-01 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for A 77-01
| M. Wt | 286.33 |
| Formula | C18H14N4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 607737-87-1 |
| PubChem ID | 10469233 |
| InChI Key | KJTYZDORHCDZPS-UHFFFAOYSA-N |
| Smiles | CC1=NC(C2=NNC=C2C3=CC=NC4=C3C=CC=C4)=CC=C1 |
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.
Solubility Data for A 77-01
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.63 | 100 | |
| 1eq. HCl | 14.32 | 50 |
Preparing Stock Solutions for A 77-01
The following data is based on the product molecular weight 286.33. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for A 77-01
References for A 77-01
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
1 Citation for A 77-01
Citations are publications that use Tocris products. Selected citations for A 77-01 include:
Vincent W et al (2020) Interplay among p21Waf1/Cip1, MUSASHI-1 and Krüppel-like factor 4 in activation of Bmi1-CreER reserve intestinal stem cells after gamma radiation-induced injury. Sci Rep 10 18300 PMID: 33110120
Do you know of a great paper that uses A 77-01 from Tocris? Please let us know.
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Literature in this Area
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Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
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.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.
Pathways for A 77-01
