A 83-01
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.
- 1. Li Yang, Xulei Wang, et al. "A tunable human intestinal organoid system achieves controlled balance between self-renewal and differentiation." Nat Commun. 2025 Jan 2;16(1):315. PMID: 39747097
- 2. Ashley N. Calder, Mirabelle Q. Peter, et al. "WNT signaling contributes to the extrahepatic bile duct proliferative response to obstruction in mice." JCI insight. December 5, 2024
- 3. Hao Ding, Zidu Xu, et al. "Kidney fibrosis molecular mechanisms Spp1 influences fibroblast activity through transforming growth factor beta smad signaling." iScience. 2024 May 9;27(9):109839. PMID: 39323737
- 4. Linlin Ji, Gongbo Fu, et al. "scRNA-seq of colorectal cancer shows regional immune atlas with the function of CD20+ B cells." Cancer Lett. 2024 Mar 1:584:216664. PMID: 38253219
- 5. Zahra Anvar, Imen Chakchouk, et al. "Comparison of Four Protocols for In Vitro Differentiation of Human Embryonic Stem Cells into Trophoblast Lineages by BMP4 and Dual Inhibition of Activin /Nodal and FGF2 Signaling." Reprod Sci. 2023 Sep 1. PMID: 37658178
- 6. XiangRong Luo, JianTao She, et al. "Establishment and characterization of organoids from a patient with adenomyoepithelioma of the breast." Bioengineered. 2021 Dec;12(2):11578-11585. PMID: 34874791
- 7. Changchun Shao, Xue Yang, et al. "The stemness of hepatocytes is maintained by high levels of lipopolysaccharide via YAP1 activation." Stem Cell Res Ther. 2021 Jun 10;12(1):342. PMID: 34112239
- 8. 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.52 |
| Cas No. | 909910-43-6 |
| Formula | C25H19N5S |
| Synonyms | A83-01; A-83-01 |
| Solubility | ≥21.1 mg/mL in DMSO; insoluble in H2O; ≥9.82 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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. |
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| Description | A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively. | |||||
| Targets | ALK5 | ALK4 | ALK7 | |||
| IC50 | 12 nM | 45 nM | 7.5 nM | |||
Quality Control & MSDS
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