APY0201

An inhibitor of PIKFYVE (IC50 = 5.2 nM); selectively inhibits IL-12 family inflammatory cytokine production (IC50s = 8, 99, and >10,000 nM for IL-12p70, IL-12p40, and TNF-α in stimulated human PBMCs); selective for PIKFYVE over a panel of 137 G protein-coupled receptors, enzymes, ion channels, and transporters, and other kinases only exhibiting >50% inhibition at LOK and ITPK1 at a concentration of 300 nM; inhibits Il-12p70 production ex vivo in murine plasma and reduces colonic inflammation in a mouse Il-10-/- cell transfer model of inflammatory bowel disease in a dose-dependent manner