A 77-01

Pricing Availability   Qty
Description: Potent inhibitor of TGF-βRI
Chemical Name: 4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline
Purity: ≥98% (HPLC)
Citations (1)
Literature (3)
Pathways (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

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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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Stem Cell Research Product Guide

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
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Stem Cells Scientific Review

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

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

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.