A 77-01
Chemical Name: 4-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]quinoline
Purity: ≥98%
Biological Activity
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).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
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The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β.
Tojo et al.
Cancer Sci., 2005;96:791 -
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain.
Sawyer et al.
J.Med.Chem., 2003;46:3953
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Citation for A 77-01
The citations listed below are publications that use Tocris products. Selected citations for A 77-01 include:
1 Citation: Showing 1 - 1
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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.
Authors: Vincent W Et al.
Sci Rep 2020;10:18300
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