5.33298

TNIK Inhibitor, KY-05009

• Synonyme(s) : TNIK Inhibitor, KY-05009, Traf2- and Nck-interacting Kinase Inhibitor, KY-05009, KY05009, 5-(4-Methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide
• Formule empirique (notation de Hill) : C₁₈H₁₆N₄O₂S
• CAS Number: 1228280-29-2
• Poids moléculaire : 352.41
• Numéro MDL: MFCD29059915
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 100 nM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: [s]1c(nc(c1NC(=O)c3ccc(cc3)C)C(=O)N)Nc2ccccc2
• Clé InChI: WCEDGRTWDSHZHF-UHFFFAOYSA-N

Description

Description générale

A cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; K_i = 100 nM, IC₅₀ = 9 nM). Also shown to inhibit the activity of MLK1 (IC₅₀ = 18 nM). Blocks multiple effects of TGF-β1 in A549 human lung adenocarcinoma cells, including nuclear translocation of β-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-β1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-β1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-β1-induced phosphorylation of focal adhesion kinase (at Tyr925), Src (at Tyr416), and paxillin (at Tyr118) and of ERK1/2 (at Thr202/Tyr204), JNK1 (Thr183/Tyr221), and JNK2 (at Thr185/Tyr223).

TNIK inhibitor, KY-05009, is a cell-permeable, highly potent inhibitor of TNIK (IC₅₀ = 9 nM). Blocks multiple effects of TGF-β1 in tumor cells.

Actions biochimiques/physiologiques

Primary Target
TNIK

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Kim, J., et al. 2014. PLOS One.9, e110180.

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
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable