For research use only. Not for therapeutic Use.
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.
| Catalog Number | I005422 |
| CAS Number | 909910-43-6 |
| Synonyms | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide |
| Molecular Formula | C₂₅H₁₉N₅S |
| Purity | ≥95% |
| Target | Anaplastic lymphoma kinase (ALK) |
| 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 |
| Reference | </br>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 </br>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 |
