A 83-01

Cat. No. 2939

A 83-01 C25H19N5S [909910-43-6]

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Chemical Name: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide

Biological Activity

Potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). Blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than SB 431542 (Cat.No. 1614). Inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.

Technical Data

M.Wt:
421.52
Formula:
C25H19N5S
Solubility:
Soluble to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
909910-43-6

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.

Certificate of Analysis / Safety Data Sheet

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Li et al (2009) Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4 16. PMID: 19097958.

Hoberg et al (2008) Attachment to laminin-111 facilitates transforming growth factor β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts. Ann.Rheum.Dis. 66 446.

Tojo et al (2005) The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer.Sci. 96 791. PMID: 16271073.

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Citations are publications that use Tocris products. Selected citations for A 83-01 include:

Zhang et al (2016) Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18 (653). PMID: 27133794.

Dai et al (2015) Maintenance and neuronal differentiation of chicken induced pluripotent stem-like cells. Stem Cells Int 2014 182737. PMID: 25610469.

Tan et al (2015) Amnion cell mediated immune modulation following bleomycin challenge: controlling the regulatory T cell response. Stem Cell Res Ther 6 8. PMID: 25634246.

Zhao et al (2015) High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling. Nat Commun 6 8243. PMID: 26354680.

O'Malley et al (2013) High-resolution analysis with novel cell-surface markers identifies routes to iPS cells. Nature 499 88. PMID: 23728301.

Okiyoneda et al (2013) Mechanism-based corrector combination restores δF508-CFTR folding and function. Nat Chem Biol 9 444. PMID: 23666117.

Yanagida et al (2013) An in vitro expansion system for generation of human iPS cell-derived hepatic progenitor-like cells exhibiting a bipotent differentiation potential. PLoS One 8 e67541. PMID: 23935837.

Telugu et al (2011) Porcine induced pluripotent stem cells analogous to naïve and primed embryonic stem cells of the mouse. Int J Dev Biol 54 1703. PMID: 21305472.

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Keywords: A 83-01, supplier, Selective, inhibitors, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK4, ALK7, ALK, Receptors, Activin, Receptor-like, Kinase, Serine/Threonine, Kinases, RSTKs, Transforming, Growth, Factor, Beta, A8301, stem, cells, growth, factors, organoids, Tocris Bioscience, TGF-β Receptor Inhibitor products

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