TNIK Inhibitor, KY-05009

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.

Primary Target
TNIK

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)