Biochem/physiol Actions
Primary TargetTNIK
General description
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.
A cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; Ki = 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).
A cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; Ki = 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).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Kim, J., et al. 2014. PLOS One.9, e110180.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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