SML0788

A 83-01

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

• Synonyme(s) : 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, A-83-01, A83-01
• Formule empirique (notation de Hill) : C₂₅H₁₉N₅S
• Numéro CAS: 909910-43-6
• Poids moléculaire : 421.52
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Nom du produit: A 83-01, ≥98% (HPLC)
• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 5 mg/mL, clear (warmed)
• Température de stockage: −20°C
• Chaîne SMILES: 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)
• Clé InChI: HIJMSZGHKQPPJS-UHFFFAOYSA-N

Description

Description générale

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.[1]

Application

A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.[2][3]

A 83-01 has been used:

• in the culture medium for organoid formation from dissociated tumor cells[4],
• as a component in Dulbecco′s modified Eagle medium/nutrient mixture F-12 (DMEM/F12) for culturing human epidermal stem cells (EpSCs)[5]

Actions biochimiques/physiologiques

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.

A-83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3