A 83-01

Tocris Bioscience, part of Bio-Techne | Catalog # 2939

(11)

Citations (943)

COA / SDS

Selective inhibitor of TGF-βRI, ALK4 and ALK7

Key Product Details

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)
Molecular Weight:	421.52

View Full Technical Details for A 83-01

Technical Data
Citations / Reviews (11)

Biological Activity for A 83-01

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. Combined with other reagents, A 83-01 promotes neural differentiation of hPSCs and also converts fibroblasts into cardiomyocytes (see protocol below).

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)

Scientific Data Examples for A 83-01

	Application of A 83-01 in Culture and Characterization of Adult Stem Cell-derived Liver Organoids. Adult stem cell-derived liver organoids were cultured using A 83-01, Y-27632 dihydrochloride (Catalog # 1254), HEPES (Catalog # 3173), Forskolin (Catalog # 1099), N-Acetylcysteine (Catalog # 7874), along with other reagents used in the human liver organoid culture protocol. After 3 days, liver organoid expansion medium was added for 7-10 days, followed by liver organoid differentiation medium, which includes A 83-01, HEPES (Catalog # 3173), Nicotinamide (Catalog # 4106), N-Acetylcysteine (Catalog # 7874), along with other reagents. Differentiated human liver organoids were stained using a (A) Human Serum Albumin Antibody (Catalog # MAB1455; red) and a (B) Human HNF-3beta /FoxA2 Antibody (Catalog # AF2400; red) and counterstained with DAPI (Catalog # 5748; blue).
	Application of A 83-01 in Culture and Characterization of iPSC-derived Human Intestinal Organoids. iPSC-derived human intestinal organoids were cultured using A 83-01, Y-27632 dihydrochloride (Catalog # 1254), SB 202190 (Catalog # 1264), N-Acetylcysteine (Catalog # 7874), Nicotinamide (Catalog # 4106), along with other reagents used in the human intestinal organoid culture protocol. (A) Human intestinal organoids were stained using a Human/Mouse/Rat Vimentin Antibody (Catalog # MAB2105; green) and a Human/Mouse Desmin Antibody (Catalog # AF3844; red) to visualize myofibroblast cells and counterstained with DAPI (Catalog # 5748; blue). (B) Human intestinal organoids were stained using a Human/Mouse E-Cadherin Antibody (Catalog # AF748; green), a Human MUC2 Antibody (Novus Biologicals, Catalog # NBP2-44431; red) and counterstained with DAPI (Catalog # 5748; blue).
	Application of A 83-01 in Culture and Characterization of Adult Stem Cell-derived Human Descending Colon Organoids. Adult stem cells isolated from human descending colon were embedded and then cultured for 30 days in intestinal organoid culture medium, which includes A 83-01, Y-27632 dihydrochloride (Catalog # 1254), SB 202190 (Catalog # 1264), N-Acetylcysteine (Catalog # 7874), Nicotinamide (Catalog # 4106), along with other reagents used in the human intestinal organoid culture protocol. (A) Organoids were fixed and stained with a Human MUC2 Antibody (Novus Biologicals; Catalog # NBP2-44431; green) to visualize intestinal goblet cells and counterstained with a Human/Mouse E-Cadherin Antibody (Catalog # AF748; red) and DAPI (Catalog # 5748; blue).(B) Organoids were fixed and stained with a Human Chromogranin A Antibody (Catalog # MAB90981; green) to visualize enteroendocrine cells and counterstained with a Human/Mouse E-Cadherin Antibody (Catalog # AF748; red) and DAPI (Catalog # 5748; blue).
	Application of A 83-01 in Culture and Characterization of Adult Stem Cell-derived Lung Organoids. Adult stem cells isolated from human lung biopsy tissue were embedded and then cultured for 20-60 days in lung organoid expansion medium, which includes A 83-01, N-Acetylcysteine (Catalog # 7874), Y-27632 dihydrochloride (Catalog # 1254), HEPES (Catalog # 3173), SB 202190 (Catalog # 1264), Nicotinamide (Catalog # 4106), along with other reagents used in the human lung organoid culture protocol. Lung organoids were able to differentiate and exhibit markers for various lung cell types. Lung organoids were stained with (A) anti-Cytokeratin 5 (KRT5) (green) and with anti-p63/TP73L (Catalog # AF1916; red) to visualize basal cells, (B) Anti-Podoplanin (PDPN) (Novus Biologicals, Catalog # NB600-1015; green) to visualize alveolar type I cells and anti- p63/TP73L (Catalog # AF1916; red) to visualize basal cells, (C, D) Anti-MUC5AC (Novus Biologicals, Catalog # NBP2-15196; green) to visualize Goblet cells and anti-SOX2 (Catalog # MAB2018; red). All samples were counterstained with DAPI (Catalog # 5748; blue).
	Application of A 83-01 in Culture and Characterization of Adult Stem Cell-derived Lung Organoids. Adult stem cells isolated from human lung biopsy tissue were embedded and then cultured for 20-60 days in lung organoid expansion medium, which includes A 83-01, N-Acetylcysteine (Catalog # 7874), Y-27632 dihydrochloride (Catalog # 1254), HEPES (Catalog # 3173), SB 202190 (Catalog # 1264), Nicotinamide (Catalog # 4106), along with other reagents used in the human lung organoid culture protocol. Lung organoids were able to differentiate and exhibit markers for various lung cell types. Lung organoids were stained with (A) anti-Cytokeratin 5 (KRT5) (green) and with anti-p63/TP73L (Catalog # AF1916; red) to visualize basal cells, (B) Anti-Podoplanin (PDPN) (Novus Biologicals, Catalog # NB600-1015; green) to visualize alveolar type I cells and anti- p63/TP73L (Catalog # AF1916; red) to visualize basal cells, (C, D) Anti-MUC5AC (Novus Biologicals, Catalog # NBP2-15196; green) to visualize Goblet cells and anti-SOX2 (Catalog # MAB2018; red). All samples were counterstained with DAPI (Catalog # 5748; blue).

Technical Data for A 83-01

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 for A 83-01

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

Preparing Stock Solutions for A 83-01

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.

Select a batch to recalculate based on the batch molecular weight:

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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References for A 83-01

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

Chen Chemically defined neural conversion of human pluripotent stem cells. Methods Mol.Biol. 2019 PMID: 30656621
Karthaus Identification of multipotent luminal progenitor cells in human prostate organoid cultures. Cells 2014 PMID: 25201529
Koehler 3D mouse embryonic stem cell culture for generating inner ear organoids. Nat.Protoc. 2014 PMID: 24784820
Jung Isolation and in vitro expansion of human colonic stem cells. Nat.Med. 2011 PMID: 21892181
Boj Organoid models of human and mouse ductal pancreatic cancer. Cell 2015 PMID: 25557080
Bartfeld In vitro expansion of human gastric epithelial stem cells and their responses to bacterial infection. Gastroenterology 2015 PMID: 25307862
Lancaster Generation of Cerebral Organoids from Human Pluripotent Stem Cells Nat.Protoc. 2015 PMID: 25188634
Mahe Establishment of gastrointestinal epithelial organoids Curr.Protoc.Mouse Biol. 2014 PMID: 25105065
Sato SnapShot: Growing Organoids from Stem Cells. Cell 2015 PMID: 26091044
Li Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 2009 PMID: 19097958
Hoberg Attachment to laminin-111 facilitates transforming growth factor β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts. Ann.Rheum.Dis. 2008 PMID: 17124250
Tojo The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer.Sci. 2005 PMID: 16271073