| Synonym(s): |
3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide; A-83-01; A83-01 |
| Formula: |
C25H19N5S |
| Application: |
A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor. |
| Color: |
White to beige |
| Storage: |
−20°C |
| Molecular Weight: |
421.52 g/mol |
| CAS Number: |
9012-63-9 |
| 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 |
| MDL number: |
MFCD00130776 |
| NACRES: |
NA.77 |
| Solubility: |
DMSO: 5 mg/mL, clear (warmed). |
| Form: |
Powder |
| Quality Level: |
300 |
| 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 |
| Assay: |
≥ 98% (HPLC) |
