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Beschreibung

TNIK inhibitor, KY-05009, is a cell-permeable, highly potent inhibitor of TNIK (IC₅,₀, = 9 nM). Blocks multiple effects of TGF-beta1 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-beta1 in A549 human lung adenocarcinoma cells, including nuclear translocation of beta-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-beta1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-beta1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-beta1-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-beta1 in A549 human lung adenocarcinoma cells, including nuclear translocation of beta-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-beta1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-beta1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-beta1-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.