SML0788

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

Properties

• 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
• 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

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3