A 83-01

A 83-01

Catalog Number:
L002368493APE
Mfr. No.:
APE-A3133
Price:
$292
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      • Overview
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          Background

          A 83-01 is a small-molecule inhibitor of activin receptorlike kinase (ALK)-5 with IC50 value of 12 nM [1].
          A 83-01 inhibited 68% of the transcriptional activation induced by ALK-5 at concentration of 1 μM in Mv1LuR4-2 cells that transfected with luciferase reporter gene and constitutively active ALK-5. In cells transfected with luciferase reporter gene only, A 83-01 treatment inhibited the activity of ALK-5 induced by TGF-β (IC50 value was 12 nM) but not BMP. A 83-01 also showed inhibition on the activity of ALK-4 and ALK-7 in R4-2 cells with IC50 values of 45 and 7.5 nM, respectively. For other ALK receptors such as ALK-1, 2, 3 and 6, A 83-01 showed weak inhibition. Besides that, A 83-01 was proved to reduce the cell growth inhibition [1].

          [1] Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer science, 2005, 96 (11): 791-800.

      • Properties
        • Alternative Name
          A83-01; A-83-01; 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
          CAS Number
          909910-43-6
          Molecular Formula
          C25H19N5S
          Molecular Weight
          421.52
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥21.1 mg/mL in DMSO; insoluble in H2O; ≥9.82 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Kathryn E. Worley, Erin E. Edwards, et al. "The importance of cell-subtype selection in creation of a 3D liver fibrosis model." Lonza Pharma&Biotech.

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