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You are here:Home-Inhibitors & Agonists-Wnt/Notch/Hedgehog-TNIK

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Wnt signaling pathways play important roles in various stages of developmental events and several aspects of adult homeostasis. Aberrant activation of Wnt signaling has also been associated with several types of cancer. We have recently identified Traf2- and Nck-interacting kinase (TNIK) as a novel activator of Wnt signaling through a comprehensive proteomic approach in human colorectal cancer cell lines.

TNIK is an activating kinase for T-cell factor-4 (TCF4) and essential for the β-catenin-TCF4 transactivation and colorectal cancer growth. Here, we report the essential role of TNIK in Wnt signaling during Xenopus development. We found that Xenopus TNIK (XTNIK) was expressed maternally and that the functional knockdown of XTNIK by catalytically inactive XTNIK (K54R) or antisense morpholino oligonucleotides resulted in significant malformations with a complete loss of head and axis structures. XTNIK enhanced β-catenin-induced axis duplication and the expression of β-catenin-TCF target genes, whereas knockdown of XTNIK inhibited it. XTNIK was recruited to the promoter region of β-catenin-TCF target genes in a β-catenin-dependent manner. These results demonstrate that XTNIK is an essential factor for the transcriptional activity of the β-catenin-TCF complex and dorsal axis determination in Xenopus embryos.

References：

1.. 2012 Oct 3; 32(40): 13987–13999.

Cat. No. Product Name CAS No. Information
H9023

LC_222150

 		886960-54-9

LC_222150 is a potent TRAF2 and NCK-Interacting Kinase(TNIK) inhibitor with IC50 value of 18.33 ± 0.75 nM use for Colorectal Cancer.
H9022

LC_64796

 		303206-05-5

LC_64796 is a potent TRAF2 and NCK-Interacting Kinase(TNIK) inhibitor with IC50 value of 18.33 ± 0.75 nM use for Colorectal Cancer.
H9021

LC_112060

 		872621-61-9

LC_112060 is a potent TRAF2 and NCK-Interacting Kinase(TNIK) inhibitor with IC50 value of 18.33 ± 0.75 nM ues for Colorectal Cancer.
H8309

NCB-0846

 		1792999-26-8

The first orally available, small-molecule TNIK inhibitor with IC50 of 21 nM; also weakly inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK (IC80>0.1 uM); induces faster migration of TCF4 phosphorylated by TNIK at 0.1-0.3 uM, and completely inhibits at 3 uM; also reduces the expression of TNIK, AXIN2, cMYC, LRP6 and LRP5; abrogates colorectal cancer stemness, suppresses Wnt-driven intestinal tumorigenesis in Apc(min/+) mice.
H8308

KY-05009

 		1228280-29-2

KY-05009 (KY05009) is a potent, ATP-competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK) with Ki of 100 nM; significantly and strongly inhibited the TGF-β-activated EMT through the attenuation of Smad and non-Smad signaling pathways, including the Wnt, NF-κB, FAK-Src-paxillin-related focal adhesion, and MAP kinases (ERK and JNK) signaling pathways in A549 cells; synergistically inhibited IL-6-stimulated proliferation and induced apoptosis through the inhibition of Wnt signaling in MM cells when combined Dovitinib.
H8311

TNIK inhibitor X

 		933886-36-3

TNIK inhibitor X is a potent inhibitor of Traf2- and Nck-interacting kinase (TNIK) (in vitro enzyme IC50=9 nM) with a reasonable selectivity over 30-folds against the majority of a panel of 50 kinases profiled; inhibits cell viability of PAMC82 and T47D cells harboring TNIK amplification with IC50 of 1.77 and 0.385 uM, respectively; shows no inhibitory activity against TNIK-non-amplified AZ-521 cells (IC50>30 uM); suppresses pAKT and induction of LC3 in TNIK-amplified PAMC82 cells, shows minimal effects on either Wnt signaling-mediated transcription.
H8310

PF-794

 		2375197-49-0

PF-794 (PF794)?is a potent, specific and ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with IC50 of 39 nM in cell-free assays; displays excellent kinome selectivity with exception of MINK1 and MAP4K4 (>60% inhibition at 1 uM); significantly inhibits TNIK-induced phosphorylation of p120-catenin, reduces pT312-immunoprecipitated p120-catenin in neurons.

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