K-756

Product NameK-756
CAS130017-40-2
MFC24H27N5O3
MW433.5
EINECS
MOL File130017-40-2.mol

Chemical Properties

Melting point	216-218 °C
Boiling point	680.0±55.0 °C(Predicted)
Density	1.261±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:4.55(Max Conc. mg/mL);10.5(Max Conc. mM)
pka	14.92±0.20(Predicted)
form	Solid
color	White to off-white

Usage And Synthesis

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_ _x000D_ 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_ _x000D_ 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.