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 (34)
Reviews (1)
Protocols (1)
Literature
Pathways

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.74 mL 23.72 mL 47.45 mL
2.5 mM 0.95 mL 4.74 mL 9.49 mL
5 mM 0.47 mL 2.37 mL 4.74 mL
25 mM 0.09 mL 0.47 mL 0.95 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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.

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Keywords: A 83-01, A 83-01 supplier, 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, BMP, and, Other, Stem, Cell, Proliferation, 2939, Tocris Bioscience

34 Citations for A 83-01

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

Liu et al (2018) CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency. Cell Stem Cell. 22 252 PMID: 29358044

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

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

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

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

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

Huang et al (2017) Zfp281 is essential for mouse epiblast maturation through transcriptional and epigenetic control of Nodal signaling. Elife 6 PMID: 29168693

Mulas et al (2017) NODAL Secures Pluripotency upon Embryonic Stem Cell Progression from the Ground State. Stem Cell Reports 9 77 PMID: 28669603

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

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

Wang et al (2016) Anti-tumor activity of SL4 against breast cancer cells: induction of G2/M arrest through modulation of the MAPK-dependent p21 signaling pathway. Sci Rep 6 36486 PMID: 27819344

Li et al (2014) PMA induces SnoN proteolysis and CD61 expression through an autocrine mechanism. Cell Signal 26 1369 PMID: 24637302

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

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

Hirschhorn et al (2012) Differential regulation of Smad3 and of the type II transforming growth factor-β receptor in mitosis: implications for signaling. PLoS One 7 e43459 PMID: 22927969

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


Do you know of a great paper that uses A 83-01 from Tocris? Please let us know.

Reviews for A 83-01

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for growing cells: Excellent publishable, performed ideally.
By Anonymous on 02/28/2019
Assay Type: In Vitro
Species: Human

used it to grow human airway basal cells


Protocols for A 83-01

The following protocol features additional information for the use of A 83-01 (Cat. No. 2939).

Literature in this Area

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

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Pathways for A 83-01

TGF-β

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.