| A 83-01 Catalog No.GC10166 |
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
| Cell experiment [1]: | |
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Cell lines |
Mv1Lu and C2C12 cells |
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Preparation method |
The solubility of this compound in DMSO is > 21.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.01 ~ 10 μM; 1 hr |
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Applications |
In Mv1Lu cells, A-83-01 reduced the level of TGF-β-induced transcription in a concentration-dependent manner, with the IC50 value of 25 nM. On the other hand, for BMP-induced transcriptional activity in C2C12 cells, A-83-01 showed no effect at the dose of 1 μM. However, at the concentrations over 3 μM, A-83-01 slightly suppressed the transcriptional activity induced by BMP4. |
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References: [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. | |
| Cas No. | 909910-43-6 | SDF | |
| Synonyms | A83-01;A-83-01 | ||
| Chemical Name | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide | ||
| Canonical SMILES | CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5 | ||
| Formula | C25H19N5S | M.Wt | 421.52 |
| Solubility | ≥21.1 mg/mL in DMSO, ≥9.82 mg/mL in EtOH with ultrasonic and warming, <2.29 mg/mL in H2O | Storage | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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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].
References:
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.