A-83-01
- CAS No.
- 909910-43-6
- Chemical Name:
- A-83-01
- Synonyms
- CS-578;A 83-01, >=98%;A 83-01;A83-01;A-83-01AB142092);ALK5 Inhibitor IV;TGF inhibitor A-83-01;A 83-01 (DMSO solution;TGF-β RI Kinase Inhibitor IV;A83-01; A-83-01;A8301;A-8301;A 8301;A 83-01, ALK4, 5 and 7 kinase inhibitor
- CBNumber:
- CB9972670
- Molecular Formula:
- C25H19N5S
- Molecular Weight:
- 421.52
- MDL Number:
- MFCD08705403
- MOL File:
- 909910-43-6.mol
- MSDS File:
- SDS
| Melting point | 111℃ |
|---|---|
| Boiling point | 590.0±60.0 °C(Predicted) |
| Density | 1.27±0.1 g/cm3(Predicted) |
| storage temp. | -20°C |
| solubility | DMSO: soluble5mg/mL, clear (warmed) |
| pka | 8.77±0.70(Predicted) |
| form | powder |
| color | white to beige |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
| FDA UNII | X3ZNM7QJ2Q |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P280-P301+P312+P330-P305+P351+P338-P337+P313 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22-36/37/38 | |||||||||
| Safety Statements | 26-36 | |||||||||
| WGK Germany | 3 | |||||||||
| NFPA 704 |
|
A-83-01 price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0788 | A 83-01 ≥98% (HPLC) | 909910-43-6 | 5mg | $93.5 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML0788 | A 83-01 ≥98% (HPLC) | 909910-43-6 | 25mg | $377 | 2024-03-01 | Buy |
| Cayman Chemical | 9001799 | A 83-01 ≥95% | 909910-43-6 | 1mg | $29 | 2024-03-01 | Buy |
| Cayman Chemical | 9001799 | A 83-01 ≥95% | 909910-43-6 | 5mg | $57 | 2024-03-01 | Buy |
| Sigma-Aldrich | 616454 | TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem | 909910-43-6 | 2mg | $216 | 2024-03-01 | Buy |
A-83-01 Chemical Properties,Uses,Production
Description
A 83-01 (909910-43-6) is a potent and selective ALK4, 5 and 7 inhibitor.1,2?IC50 = 45, 12 and 7.5 nM respectively. Prevents phosphorylation of Smad2/3 and growth inhibition induced by TGFβ.2?Inhibits differentiation of rat induced pluripotent stem cells and increases clonal expansion efficiency.3?Together with AMI-5, A83-01 enabled Oct4-induced reprogramming of mouse embryonic fibroblasts.4?Cell permeable. Active in vivo.
Uses
A 83-01 is a selective inhibitor of TGF-β type I receptor. A 83-01 treatment increases tumor permeability.
Uses
A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.
Biological Activity
Selective inhibitor of TGF- β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC 50 values are 12, 45 and 7.5 nM respectively). Blocks phosphorylation of Smad2 and inhibits TGF- β -induced epithelial-to-mesenchymal transition. Only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. More potent than SB 431542 (4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol -2-yl]benzamide). Inhibits differentiation of rat induced pluripotent stem cells (riPSCs) and increases clonal expansion efficiency. Helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.
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.
Enzyme inhibitor
This TGFb inhibitor (FW = 421.52 g/mol; CAS 909910-43-6; Solubility: 50 mM in DMSO), named 3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, selectively targets TGF-β type I receptor ALK5 kinase (IC50 = 12 nM), Type I Activin/Nodal receptor ALK4 (IC50 = 45 nM), and type I nodal receptor ALK7 (IC50 = 7.5 nM), blocking the phosphorylation of Smad2 and inhibiting TGF-β-induced epithelial-to-mesenchymal transitions. TGF-β signaling inhibitors represent a useful strategy for treating patients with tumor growth and metastasis in advanced cancer. A-83-01 only weakly inhibits ALK-1, ALK-2, ALK-3, ALK-6 and MAPK. It also has little or no effect on bone morphogenetic protein type I receptors, p38 mitogen-activated protein kinase, or extracellular regulated kinase. A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Its use also instrumental in demonstrating that attachment to Laminin-111 facilitates TGF-β-induced expression of matrix metalloproteinase-2 in synovial fibroblasts.
storage
-20°C (protect from light)
References
1) Vogt. et al. (2011), The specificities of small molecule inhibitors of the TGFβ and BMP pathways; Cell Signal., 23 1831 2) Tojo et al. (2012), Characteristic differences among osteogenic cell populations of rat bone marrow stromal cells isolated from untreated, hemolyzed or Ficoll-treated marrow; Cancer Sci., 96 791 3) Li et al. (2009), Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors; Cell Stem Cell, 4 16 4) Yuan et al. (2011), Brief report: combined chemical treatment enables Oct4-induced reprogramming from mouse embryonic fibroblasts; Stem Cells, 29 549
A-83-01 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32956 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30238 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
| Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9984 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38631 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
