TNIK-IN-5

TNIK-IN-5 is an efficient TNIK inhibitor with IC50 of 0.05 μM. TNIK-IN-5 efficiently inhibits Wnt signaling in intact cells. TNIK-IN-5 shows excellent in vitro anti-colorectal cancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Wnt

IC50: 0.05 μM (TNIK)[1]

TNIK-IN-5 (compound 8g) (1.25-5 μM; 48 hours) significantly inhibits the cell proliferation of HCT116 in a dose-dependent manner[1]. TNIK-IN-5 (1 μM; 24, 48 hours) strongly prevents HCT116 cells migration[1]. TNIK-IN-5 (10-40 μM; 48 hours) concentration-dependently inhibits the protein levels of β-catenin and TCF-4 in the nucleus, and significantly decreases the expression of Wnt target gene products, including Axin2 and c-Myc[1]. Cell Proliferation Assay Cell Line: HCT116 cells[1] Concentration: 1.25 μM, 2.5 μM, 5 μM Incubation Time: 48 hours Result: Significantly inhibited the cell proliferation in a dose-dependent manner.

[1]. Luo X, Yang R, Li Y, Zhang L, Yang S, Li L. Discovery of benzo[d]oxazol-2(3H)-one derivatives as a new class of TNIK inhibitors for the treatment of colorectal cancer. Bioorg Med Chem Lett. 2022;67:128745.