LGK974 is a potent and selective inhibitor of Porcupine (IC50 = 1 nM). Inhibits Wnt signaling (IC50 = 0.4 nM) in vitro and in vivo.1 It displays efficacy in several cancer models including glioblastoma2,6, squamous cell3, renal cell carcinoma4, and non-small cell lung5. LGK974 reprogrammed the immune suppressive tumor microenvironment in a mouse model of glioblastoma to increase antitumor immune responses.6 It also potentiated anti-PD1 therapy by increasing DC3-like dendritic cells and decreasing myeloid suppressor cells. LGK974 attenuated myocardial ischemia-reperfusion injury by reducing inflammatory responses.7
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