A 83-01

Catalog # Availability Size / Price Qty
A 83-01 | CAS No. 909910-43-6 | TGF-beta Receptor Inhibitors
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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%

Product Details
Citations (83)
Supplemental Products

Biological Activity

A 83-01 is a 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). A 83-01 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). A 83-01 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. Also promotes neural differentiation of hPSCs as part of a chemical cocktail.

A 83-01 synthesized to Ancillary Material Grade also available.

For more information about how A 83-01 may be used, see our protocol: Converting Fibroblasts into Cardiomyocytes (9C Cocktail)

Technical Data

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

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.

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Citations for A 83-01

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

83 Citations: Showing 1 - 10

  1. FOXA2 drives lineage plasticity and KIT pathway activation in neuroendocrine prostate cancer.
    Authors: Han Et al.
    Cancer Cell  2022;40:1306
  2. Optimized human intestinal organoid model reveals interleukin-22-dependency of paneth cell formation.
    Authors: He Et al.
    Cell Stem Cell  2022;29:1333
  3. An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection.
    Authors: Duan Et al.
    Cell Rep.  2021;37:109920
  4. Global phosphoproteomics reveal CDK suppression as a vulnerability to KRas addiction in pancreatic cancer.
    Authors: Kazi Et al.
    Clin Cancer Res  2021;27:4012
  5. A versatile polypharmacology platform promotes cytoprotection and viability of human pluripotent and differentiated cells.
    Authors: Chen Et al.
    Nat.Methods  2021;18:528
  6. Microenvironment drives cell state, plasticity, and drug response in pancreatic cancer.
    Authors: Raghavan Et al.
    Cell  2021;184:6119
  7. Robotic high-throughput biomanufacturing and functional differentiation of human pluripotent stem cells.
    Authors: Tristan Et al.
    Stem Cell Rep  2021;16:3076
  8. Critical Role of Type III Interferon in Controlling SARS-CoV-2 Infection in Human Intestinal Epithelial Cells
    Authors: Stanifer Et al.
    Cell Rep  2020;32:107863
  9. Snake venom gland organoids.
    Authors: Post Et al.
    Cell  2020;180:233
  10. Immunoevolution of mouse pancreatic organoid isografts from preinvasive to metastatic disease.
    Authors: Filippini Et al.
    Sci Rep  2019;9:12286
  11. Evaluating Shigella flexneri Pathogenesis in the Human Enteroid Model.
    Authors: Ranganathan Et al.
    Infect Immun  2019;87
  12. Sera Antibody Repertoire Analyses Reveal Mechanisms of Broad and Pandemic Strain Neutralizing Responses after Human Norovirus Vaccination.
    Authors: Lindesmith Et al.
    Immunity  2019;50:1530
  13. Expansion of Luminal Progenitor Cells in the Aging Mouse and Human Prostate.
    Authors: Crowell Et al.
    Cell Rep  2019;28:1499
  14. Establishment of Patient-Derived Organoids and Drug Screening for Biliary Tract Carcinoma.
    Authors: Saito Et al.
    Cell Rep  2019;27:1265
  15. Rectal Organoids Enable Personalized Treatment of Cystic Fibrosis.
    Authors: Berkers Et al.
    Cell Rep  2019;26:1701
  16. Establishment and Morphological Characterization of Patient-Derived Organoids from Breast Cancer.
    Authors: Mazzucchelli Et al.
    Biol Proced Online  2019;21:12
  17. Conserved regulation of RNA processing in somatic cell reprogramming.
    Authors: Kanitz Et al.
    BMC Genomics  2019;20:100
  18. Development of Collagen-Based 3D Matrix for Gastrointestinal Tract-Derived Organoid Culture.
    Authors: Jee Et al.
    Stem Cells Int  2019;2019:8472712
  19. Folding-function relationship of the most common cystic fibrosis-causing CFTR conductance mutants.
    Authors: Willigen Et al.
    Life Sci Alliance  2019;2
  20. Chemically Defined Neural Conversion of Human Pluripotent Stem Cells
    Authors: Chen Et al.
    Methods Mol.Biol.  2019;1919:59
  21. Capacitation of human na�ve pluripotent stem cells for multi-lineage differentiation.
    Authors: Rostovskaya Et al.
    Development  2019;146
  22. Activin Is Superior to BMP7 for Efficient Maintenance of Human iPSC-Derived Nephron Progenitors.
    Authors: Tanigawa Et al.
    Stem Cell Reports  2019;13:322
  23. Activating a Reserve Neural Stem Cell Population In Vitro Enables Engraftment and Multipotency after Transplantation.
    Authors: Peterson Et al.
    Stem Cell Reports  2019;12:680
  24. Role of cyclooxygenase-2-mediated prostaglandin E2-prostaglandin E receptor 4 signaling in cardiac reprogramming.
    Authors: Muraoka Et al.
    Nat Commun  2019;10:674
  25. Human Intestinal Enteroids Model MHC-II in the Gut Epithelium.
    Authors: Wosen Et al.
    Front Immunol  2019;10:1970
  26. LRH-1 mitigates intestinal inflammatory disease by maintaining epithelial homeostasis and cell survival.
    Authors: Bayrer Et al.
    Nat Commun  2018;9:4055
  27. A stably self-renewing adult blood-derived induced neural stem cell exhibiting patternability and epigenetic rejuvenation.
    Authors: Sheng Et al.
    Nat Commun  2018;9:4047
  28. Morphological alterations of cultured human colorectal matched tumour and healthy organoids.
    Authors: Kashfi Et al.
    Oncotarget  2018;9:10572
  29. Expansion of Airway Basal Cells and Generation of Polarized Epithelium.
    Authors: Levardon Et al.
    Bio Protoc  2018;8
  30. COX-2-PGE2 Signaling Impairs Intestinal Epithelial Regeneration and Associates with TNF Inhibitor Responsiveness in Ulcerative Colitis.
    Authors: Li Et al.
    EBioMedicine  2018;36:497
  31. Development and Characterization of Human Cerebral Organoids: An Optimized Protocol.
    Authors: Yakoub and Sadek
    Cell Transplant  2018;27:393
  32. Single-Cell Analysis Identifies LY6D as a Marker Linking Castration-Resistant Prostate Luminal Cells to Prostate Progenitors and Cancer.
    Authors: Barros-Silva Et al.
    Cell Rep  2018;25:3504
  33. Super-Obese Patient-Derived iPSC Hypothalamic Neurons Exhibit Obesogenic Signatures and Hormone Responses.
    Authors: Rajamani Et al.
    Cell Stem Cell  2018;22:698
  34. Myoepithelial Cells of Submucosal Glands Can Function as Reserve Stem Cells to Regenerate Airways after Injury.
    Authors: Tata Et al.
    Cell Stem Cell  2018;22:668
  35. Submucosal Gland Myoepithelial Cells Are Reserve Stem Cells That Can Regenerate Mouse Tracheal Epithelium.
    Authors: Lynch Et al.
    Cell Stem Cell  2018;22:653
  36. CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency.
    Authors: Liu Et al.
    Cell Stem Cell.  2018;22:252
  37. Inflammatory Cytokine TNFα Promotes the Long-Term Expansion of Primary Hepatocytes in 3D Culture.
    Authors: Peng Et al.
    Cell  2018;175:1607
  38. Colon organoid formation and cryptogenesis are stimulated by growth factors secreted from myofibroblasts.
    Authors: Yip Et al.
    PLoS One  2018;13:e0199412
  39. Colonoscopy-based colorectal cancer modeling in mice with CRISPR-Cas9 genome editing and organoid transplantation.
    Authors: Roper Et al.
    Nat Protoc  2018;13:217
  40. IL-1-induced JAK/STAT signaling is antagonized by TGF-beta to shape CAF heterogeneity in pancreatic ductal adenocarcinoma.
    Authors: Biffi Et al.
    Cancer Discov  2018;
  41. NODAL Secures Pluripotency upon Embryonic Stem Cell Progression from the Ground State.
    Authors: Mulas Et al.
    Stem Cell Reports  2017;9:77
  42. Enhanced Development of Skeletal Myotubes from Porcine Induced Pluripotent Stem Cells.
    Authors: Genovese
    Sci Rep  2017;7:41833
  43. Zfp281 is essential for mouse epiblast maturation through transcriptional and epigenetic control of Nodal signaling.
    Authors: Huang Et al.
    Elife  2017;6
  44. Organoid culture of human prostate cancer cell lines LNCaP and C4-2B.
    Authors: Ma Et al.
    Am J Clin Exp Urol  2017;5:25
  45. Establishment of mouse expanded potential stem cells.
    Authors: Yang Et al.
    Nature  2017;550:393
  46. In vivo genome editing and organoid transplantation models of colorectal cancer and metastasis.
    Authors: Roper Et al.
    Nat Biotechnol  2017;35:569
  47. Induced Pluripotent Stem Cell-Derived Dopaminergic Neurons from Adult Common Marmoset Fibroblasts.
    Authors: Vermilyea Et al.
    Stem Cells Dev  2017;26:1225
  48. Constitutively Active SMAD2/3 Are Broad-Scope Potentiators of Transcription-Factor-Mediated Cellular Reprogramming.
    Authors: Ruetz Et al.
    Cell Stem Cell  2017;21:791
  49. Enhancer Reprogramming Promotes Pancreatic Cancer Metastasis.
    Authors: Roe Et al.
    Cell  2017;170:875
  50. Epigenetic resetting of human pluripotency.
    Authors: Guo Et al.
    Development  2017;144:2748
  51. Immunopathology of childhood celiac disease-Key role of intestinal epithelial cells.
    Authors: Pietz Et al.
    PLoS One  2017;12:e0185025
  52. Anti-tumor activity of SL4 against breast cancer cells: induction of G2/M arrest through modulation of the MAPK-dependent p21 signaling pathway.
    Authors: Wang Et al.
    Sci Rep  2016;6:36486
  53. Angiopoietin-like 4 promotes angiogenesis in the tendon and is increased in cyclically loaded tendon fibroblasts.
    Authors: Mousavizadeh Et al.
    J Physiol  2016;594:2971
  54. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell  2016;19:217
  55. Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation.
    Authors: Zhang Et al.
    Cell Stem Cell  2016;18(653)
  56. Human Enteroids as a Model of Upper Small Intestinal Ion Transport Physiology and Pathophysiology.
    Authors: Foulke-Abel Et al.
    Nat Protoc  2016;150:638
  57. Inhibition of TGFβ cell signaling for limbal explant culture in serumless, defined xeno-free conditions.
    Authors: Zamudio Et al.
    Exp Eye Res  2016;145:48
  58. Organoid culture systems for prostate epithelial and cancer tissue.
    Authors: Drost Et al.
    Proc Natl Acad Sci U S A  2016;11:347
  59. High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling.
    Authors: Zhao Et al.
    Nat Commun  2015;6:8243
  60. Amnion cell mediated immune modulation following bleo. challenge: controlling the regulatory T cell response.
    Authors: Tan Et al.
    Stem Cell Res Ther  2015;6:8
  61. Disease Modeling and Gene Therapy of Copper Storage Disease in Canine Hepatic Organoids.
    Authors: Nantasanti Et al.
    Stem Cell Res  2015;5:895
  62. CPM Is a Useful Cell Surface Marker to Isolate Expandable Bi-Potential Liver Progenitor Cells Derived from Human iPS Cells.
    Authors: Kido Et al.
    Inflamm Bowel Dis  2015;5:508
  63. Transcription factor binding dynamics during human ES cell differentiation.
    Authors: Tsankov Et al.
    Stem Cell Reports  2015;518:344
  64. Targeted disruption of DNMT1, DNMT3A and DNMT3B in human embryonic stem cells.
    Authors: Liao Et al.
    Cell  2015;47:469
  65. TGFβ loss activates ADAMTS-1-mediated EGF-dependent invasion in a model of esophageal cell invasion.
    Authors: Bras Et al.
    Nat Genet  2015;330:29
  66. HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity.
    Authors: Mattis Et al.
    Exp Cell Res  2015;24:3257
  67. Microbial Disruption of Autophagy Alters Expression of the RISC Component AGO2, a Critical Regulator of the miRNA Silencing Pathway.
    Authors: Sibony Et al.
    Proc Natl Acad Sci U S A  2015;21:2778
  68. Maintenance and neuronal differentiation of chicken induced pluripotent stem-like cells.
    Authors: Dai Et al.
    Stem Cells Int  2015;2014:182737
  69. Organoid models of human and mouse ductal pancreatic cancer.
    Authors: Boj Et al.
    Cell  2015;160:324
  70. Long-term culture of genome-stable bipotent stem cells from adult human liver.
    Authors: Huch Et al.
    Nature  2015;160:299
  71. Heightened potency of human pluripotent stem cell lines created by transient BMP4 exposure.
    Authors: Yang Et al.
    Stem Cell Reports  2015;112:E2337
  72. Preserved genetic diversity in organoids cultured from biopsies of human colorectal cancer metastases.
    Authors: Weeber Et al.
    Hum Mol Genet  2015;112:13308
  73. PMA induces SnoN proteolysis and CD61 expression through an autocrine mechanism.
    Authors: Li Et al.
    Cell Signal  2014;26:1369
  74. β-Cell differentiation of human pancreatic duct-derived cells after in vitro expansion.
    Authors: Corritore Et al.
    Cell Cycle  2014;16:456
  75. Mechanism-based corrector combination restores δF508-CFTR folding and function.
    Authors: Okiyoneda Et al.
    Nat Chem Biol  2013;9:444
  76. Generation of BAC transgenic epithelial organoids.
    Authors: Schwank Et al.
    Cell Reprogram  2013;8:e76871
  77. An in vitro expansion system for generation of human iPS cell-derived hepatic progenitor-like cells exhibiting a bipotent differentiation potential.
    Authors: Yanagida Et al.
    PLoS One  2013;8:e67541
  78. High-resolution analysis with novel cell-surface markers identifies routes to iPS cells.
    Authors: O'Malley Et al.
    Nature  2013;499:88
  79. Immunosurveillance against tetraploidization-induced colon tumorigenesis.
    Authors: Boilàve Et al.
    Proc Natl Acad Sci U S A  2013;12:473
  80. Generation of organized anterior foregut epithelia from pluripotent stem cells using small molecules.
    Authors: Kearns Et al.
    PLoS One  2013;11:1003
  81. Differential regulation of Smad3 and of the type II transforming growth factor-β receptor in mitosis: implications for signaling.
    Authors: Hirschhorn Et al.
    PLoS One  2012;7:e43459
  82. Porcine induced pluripotent stem cells analogous to naïve and primed embryonic stem cells of the mouse.
    Authors: Telugu Et al.
    Int J Dev Biol  2011;54:1703
  83. Generation of genetically modified rats from embryonic stem cells.
    Authors: Kawamata and Ochiya
    Nature  2010;107:14223


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