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

Soluble to 50 mM in DMSO
>98 %
Store at -20°C

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:

Drost et al (2016) Organoid culture systems for prostate epithelial and cancer tissue. Proc Natl Acad Sci U S A 11 347. PMID: 26797458.

Foulke-Abel et al (2016) Human Enteroids as a Model of Upper Small Intestinal Ion Transport Physiology and Pathophysiology. Nat Protoc 150 638. PMID: 26677983.

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217. PMID: 27320041.

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

Boj et al (2015) Organoid models of human and mouse ductal pancreatic cancer. Cell 160 324. PMID: 25557080.

Bras et al (2015) TGFβ loss activates ADAMTS-1-mediated EGF-dependent invasion in a model of esophageal cell invasion. Nat Genet 330 29. PMID: 25064463.

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

Huch et al (2015) Long-term culture of genome-stable bipotent stem cells from adult human liver. Nature 160 299. PMID: 25533785.

Kido et al (2015) CPM Is a Useful Cell Surface Marker to Isolate Expandable Bi-Potential Liver Progenitor Cells Derived from Human iPS Cells. Inflamm Bowel Dis 5 508. PMID: 26365514.

Liao et al (2015) Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells. Cell 47 469. PMID: 25822089.

Mattis et al (2015) HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity. Exp Cell Res 24 3257. PMID: 25740845.

Nantasanti et al (2015) Disease Modeling and Gene Therapy of Copper Storage Disease in Canine Hepatic Organoids. Stem Cell Res 5 895. PMID: 26455412.

Sibony et al (2015) Microbial Disruption of Autophagy Alters Expression of the RISC Component AGO2, a Critical Regulator of the miRNA Silencing Pathway. Proc Natl Acad Sci U S A 21 2778. PMID: 26332312.

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.

Tsankov et al (2015) Transcription factor binding dynamics during human ES cell differentiation. Stem Cell Reports 518 344. PMID: 25693565.

Weeber et al (2015) Preserved genetic diversity in organoids cultured from biopsies of human colorectal cancer metastases. Hum Mol Genet 112 13308. PMID: 26460009.

Yang et al (2015) Heightened potency of human pluripotent stem cell lines created by transient BMP4 exposure. Stem Cell Reports 112 E2337. PMID: 25870291.

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

Corritore et al (2014) β-Cell differentiation of human pancreatic duct-derived cells after in vitro expansion. Cell Cycle 16 456. PMID: 25437872.

Boilàve et al (2013) Immunosurveillance against tetraploidization-induced colon tumorigenesis. Proc Natl Acad Sci U S A 12 473. PMID: 23324343.

Kearns et al (2013) Generation of organized anterior foregut epithelia from pluripotent stem cells using small molecules. PLoS One 11 1003. PMID: 23917481.

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.

Schwank et al (2013) Generation of BAC transgenic epithelial organoids. Cell Reprogram 8 e76871. PMID: 24204693.

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.

Kawamata and Ochiya (2010) Generation of genetically modified rats from embryonic stem cells. Nature 107 14223. PMID: 20660726.

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