ChemicalBook > CAS DataBase List > A-83-01

A-83-01

Product Name
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
Formula Weight
421.52
MOL File
909910-43-6.mol
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A-83-01 Property

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)
form 
powder
pka
8.77±0.70(Predicted)
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.
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Safety

Hazard Codes 
Xn
Risk Statements 
22-36/37/38
Safety Statements 
26-36
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0788
Product name
A 83-01
Purity
≥98% (HPLC)
Packaging
5mg
Price
$93.5
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0788
Product name
A 83-01
Purity
≥98% (HPLC)
Packaging
25mg
Price
$377
Updated
2024/03/01
Cayman Chemical
Product number
9001799
Product name
A 83-01
Purity
≥95%
Packaging
1mg
Price
$29
Updated
2024/03/01
Cayman Chemical
Product number
9001799
Product name
A 83-01
Purity
≥95%
Packaging
5mg
Price
$57
Updated
2024/03/01
Sigma-Aldrich
Product number
616454
Product name
TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
Packaging
2mg
Price
$216
Updated
2024/03/01
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A-83-01 Chemical Properties,Usage,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

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A-83-01 Suppliers

Americas 1 Canada 1 China 93 Europe 1 India 1 Japan 1 Switzerland 1 United Kingdom 3 United States 21 Global 123
AdooQ BioScience, LLC
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909910-43-6, A-83-01Related Search:

(E)-2-cyano-3-(4-hydroxy-3,5-diisopropylphenyl)-N-(3-phenylpropyl)acrylamide TYRPHOSTIN AG 879 6-[4-(2-PIPERIDIN-1-YLETHOXY)PHENYL]-3-PYRIDIN-4-YLPYRAZOLO[1,5-A]PYRIMIDINE LM 22A4 Deionized water (2R,3S/2S,3R)-3-(4-Chloro-5-fluoro-6-pyrimidinyl)-2-(2,4-difluorophenyl)butan-2-ol hydrochloride 4-[3-(6-METHYL-2-PYRIDINYL)-1H-PYRAZOL-4-YL]-QUINOLINE A-83-01 LY-364947

  • 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
  • A 83-01;A83-01
  • TGF inhibitor A-83-01
  • 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
  • TGF-β RI Kinase Inhibitor IV
  • A-83-01AB142092)
  • ALK5 Inhibitor IV
  • A 83-01, >=98%
  • 1H-Pyrazole-1-carbothioamide,3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-
  • 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
  • A83-01; A-83-01;A8301;A-8301;A 8301
  • TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
  • CS-578
  • A 83-01 (DMSO solution
  • 3-(6-Methyl-2-pyridyl)-N-phenyl-4-(4-quinolinyl)pyrazole-1-carbothioamide
  • A 83-01, ALK4, 5 and 7 kinase inhibitor
  • 909910-43-6
  • C25H19N5S
  • Inhibitors
  • TGF-beta/Smad
  • Protein Kinase