A 83-01

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Cat.No. 2939 - A 83-01 | C25H19N5S | CAS No. 909910-43-6
Description: Selective inhibitor of TGF-βRI, ALK4 and ALK7
Chemical Name: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
Purity: ≥98% (HPLC)
Datasheet
Citations (28)

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.

Compound Libraries

A 83-01 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 421.52
Formula C25H19N5S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 909910-43-6
PubChem ID 16218924
InChI Key HIJMSZGHKQPPJS-UHFFFAOYSA-N
Smiles S=C(NC5=CC=CC=C5)N(N=C3C4=NC(C)=CC=C4)C=C3C2=CC=NC1=CC=CC=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.08 50

Preparing Stock Solutions

The following data is based on the product molecular weight 421.52. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.37 mL 11.86 mL 23.72 mL
5 mM 0.47 mL 2.37 mL 4.74 mL
10 mM 0.24 mL 1.19 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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 PMID:

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


If you know of a relevant reference for A 83-01, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: Selective inhibitors inhibits 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 TGF-beta Receptors

28 Citations for A 83-01

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

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

Genovese (2017) Enhanced Development of Skeletal Myotubes from Porcine Induced Pluripotent Stem Cells. Sci Rep 7 41833 PMID: 28165492

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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