Description
K-756 is a a selective Wnt/β-catenin pathway inhibitor. K-756 is also a tankyrase (TNKS) inhibitor. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. could be a leading compound in the development of anticancer agents.
in vitro
K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. Moreover, PARP family enzyme assays showed that K-756 is a selective TNKS inhibitor. K-756 inhibited the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. _x000D_
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Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/
in vivo
An in vivo study showed that the oral administration of K-756 inhibited the Wnt/β-catenin pathway in colon cancer xenografts in mice._x000D_
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Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/
target
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TMS1 amd TMLS2 with IC50s of 31 and 36 nM, respectively.
