616454

A 83-01

≥97% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem

• Synonyme(s) : TGF-β RI Kinase Inhibitor IV, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor IV, 3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole, A-83-01, ALK5 Inhibitor IV
• Formule empirique (notation de Hill) : C₂₅H₁₉N₅S
• CAS Number: 909910-43-6
• Poids moléculaire : 421.52
• Numéro MDL: MFCD08705403
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.54

Propriétés

• Product Name: TGF-β RI Kinase Inhibitor IV, TGF-β RI Kinase Inhibitor IV, CAS 909910-43-6, is a cell-permeable, selective inhibitor of ALK-4/5/7-mediated signaling (IC₅₀ = 45, 12, and 7.5 nM, respectively).
• Niveau de qualité: 200
• Essai: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: pale yellow
• Solubilité: DMSO: 20 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1
• InChI: 1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
• Clé InChI: HIJMSZGHKQPPJS-UHFFFAOYSA-N

Description

Description générale

A cell-permeable trisubstituted pyrazole compound that has been shown to selectively inhibit ALK-4/5/7-mediated (IC₅₀ = 45, 12, and 7.5 nM, respectively, in luciferase transcription activity assays), but not ALK-1/2/3/6-mediated cellular signaling in Mv1Lu R4-2 transfectants expressing the individual Type I TGF-β receptors. Inhibits TGF-β-induced Smad2-phosphorylation in HaCaT cells and epithelial-to-mesenchymal transition in NMuMG cells at a concentration of 1 µM.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
ALK-4/5/7

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 45, 12, and 7.5 nM, respectively, in inhibit ALK-4/5/7-mediated luciferase transcription activity assays

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Tojo, M., et al. 2005. Cancer Sci.96, 791.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3