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SML0788

Sigma-Aldrich

A 83-01

≥98% (HPLC), powder, TGF-β RI kinase inhibitor

Synonym(s):

3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, A-83-01, A83-01

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About This Item

Empirical Formula (Hill Notation):
C25H19N5S
CAS Number:
909910-43-6
Molecular Weight:
421.52
UNSPSC Code:
12352200
NACRES:
NA.77

Product Name

A 83-01, ≥98% (HPLC)

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1

InChI

1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)

InChI key

HIJMSZGHKQPPJS-UHFFFAOYSA-N

General description

A-83-01 may effectively prevent burn wound contraction without impeding wound closure, due to its ability to inhibit the transforming growth factor-β (TGF-β)-induced rise in myofibroblast population. Additionally, it can hinder TGF-β1-dependent cancer metastasis by suppressing epithelial-mesenchymal transition (EMT) in animals.

Application

A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.
A 83-01 has been used:
  • in the culture medium for organoid formation from dissociated tumor cells,
  • as a component in Dulbecco′s modified Eagle medium/nutrient mixture F-12 (DMEM/F12) for culturing human epidermal stem cells (EpSCs)

Biochem/physiol Actions

A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
0000383524
0000383524
0000369551
0000369550
0000257827

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A83-01 inhibits TGF-Β-induced upregulation of Wnt3 and epithelial to mesenchymal transition in HER2-overexpressing breast cancer cells.
Wu Y, et al.
Breast Cancer Research and Treatment, 163(3), 449-460 (2017)
Personalized identification of optimal HIPEC perfusion protocol in patient-derived tumor organoid platform
Forsythe SD, et al.
Annals of Surgical Oncology, 27, 4950-4960 (2020)
Topical application of ALK5 inhibitor A-83-01 reduces burn wound contraction in rats by suppressing myofibroblast population
Sun X, et al.
Bioscience, Biotechnology, and Biochemistry, 78, 1805-1812 (2014)
The Use of Endometrial Cancer Patient?Derived Organoid Culture for Drug Sensitivity Testing Is Feasible
Girda E, et al.
International Journal of Gynecological Cancer : Official Journal of the International Gynecological Cancer Society, 27(8), 1701-1701 (2017)
Eugenia Girda et al.
International journal of gynecological cancer : official journal of the International Gynecological Cancer Society, 27(8), 1701-1707 (2017-07-07)
Patient-derived organoids (PDOs), used in multiple tumor types, have allowed evaluation of tumor characteristics from individual patients. This study aimed to assess the feasibility of applying PDO in vitro culture for endocrine-based and drug sensitivity testing in endometrial cancer. Endometrial
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