A 83-01

• CAT Number: I005422
• CAS Number: 909910-43-6
• Molecular Formula: C₂₅H₁₉N₅S
• Molecular Weight: 421.52
• Purity: ≥95%
• Target: TGF-βR1(ALK5)
• Solubility: 50 mM in DMSO
• Storage: Store at -20°C
• IC50: 12 nM ( ALK5)
• IUPAC Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
• InChI: 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)
• InChIKey: HIJMSZGHKQPPJS-UHFFFAOYSA-N
• SMILES: CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5

A 83-01 (Cat.No:I005422), also known as N-[trans-4-[(4-Fluorophenyl)thiazol-2-yl]cyclohexyl]-4-morpholinobenzenesulfonamide, is a potent inhibitor of TGF-β type I receptor kinase (ALK5) with an IC50 of 12 nM. It also inhibits other kinases, including ALK4 and ALK7, but at higher concentrations. A 83-01 has been shown to suppress the differentiation of embryonic stem cells, induce epithelial-to-mesenchymal transition, and inhibit tumor growth.

Reference

1:Topical application of ALK5 inhibitor A-83-01 reduces burn wound contraction in rats by suppressing myofibroblast population. Sun X, Kim YH, Phan TN, Yang BS.Biosci Biotechnol Biochem. 2014;78(11):1805-12. doi: 10.1080/09168451.2014.932666. Epub 2014 Jul 10. PMID: 25351330 2:The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T.Cancer Sci. 2005 Nov;96(11):791-800. PMID: 16271073 Free Article