KY 02111 is a selective inhibitor of Wnt may by targeting the downstream from GSK3βand APC in β-catenin destruction complex [1].
Wnt signaling pathways are a group of signal transduction pathways made of proteins and play an important role in passing signals from outside of a cell through cell surface receptors to the inside of the cell. Wnt signaling initially was identified as a pivotal mediator in carcinogenesis, but has since been recognized for its function in embryonic development, including body axis patterning, cell fate specification, cell proliferation, and cell migration which are necessary for proper formation of important tissues including bone, heart, and muscle [2].
KY 02111 is a potent Wnt inhibitor and has a different selectivity with the reported Wnt inhibitors. When tested with IMR90-1 hiPSCs transfected with TCF receptor plasmids, KY 02111 (1 μM) significantly reduced luciferase activities in a dose-dependent manner by inhibiting canonical WNT signaling pathway. In cardiac colonies on the day 30, KY 02111 showed that nearly 73%-85% of IMR90-1 hiPSCs expressed the cardiac markers [1].
References:
[1]. Minami, I., et al., A small molecule that promotes cardiac differentiation of human pluripotent stem cells under defined, cytokine- and xeno-free conditions. Cell Rep, 2012. 2(5): p. 1448-60.
[2]. Stamatakou, E., M. Hoyos-Flight, and P.C. Salinas, Wnt Signalling Promotes Actin Dynamics during Axon Remodelling through the Actin-Binding Protein Eps8. PLoS One, 2015. 10(8): p. e0134976.