WEE1 kinase has been reported to be aberrantly expressed in melanomas, glioblastoma multiforme (GBMs), triple negative breast cancers (TNBCs) and some prostate cancers. Dependence of various cancer cells on WEE1 signaling suggests that targeting epigenentic activity of WEE1 is a viable strategy for overcoming tumor proliferation.
Recently, we designed a novel assay that provides specific and quantitative measure of WEE1 epigenetic activity. Using this assay, we have screened the libraries and have identified two new scaffolds, both of which are highly efficient in suppressing WEE1 epigenetic activity. These two new class of WEE1 inhibitors not only suppress WEE1 kinase activity, but also have shown propensity to overcome WEE1 mediated cell cycle regulation.
Feel free to contact us if you are interested in exploring these inhibitors in your system.