A-83-01

ChemicalBook > CAS DataBase List > 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;TGF-β RI Kinase Inhibitor IV - CAS 909910-43-6 - Calbiochem
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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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

909910-43-6

C25H19N5S

Inhibitors

TGF-beta/Smad

Protein Kinase