map4k4-in-3

MAP4K4-IN-3 (Compound 17), a serine/threonine protein kinase, may be a viable target for antidiabetic agents.

PI4K-IN-3 (Compound 27) is an orally effective PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. It does not inhibit the hERG channel and is non-cytotoxic to mammalian cells. This compound shows notable selectivity for human MINK1 and MAP4K4 kinases but has lower selectivity for human PI3Kα and PI4Kβ. PI4K-IN-3 exhibits potent antimalarial activity, significantly reducing parasitemia in NSG mouse models infected with Plasmodium falciparum.

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].