APY0201

APY0201 is an inhibitor of FYVE finger-containing phosphoinositide kinase (PIKFYVE, IC50 = 5.2 nM) that selectively inhibits interleukin-12 (IL-12) family inflammatory cytokine production (IC50s = 8, 99, and >10,000 nM for IL-12p70, IL-12p40, and TNF-alpha in stimulated human peripheral blood mononuclear cells (PBMCs)). It is selective for PIKFYVE over a panel of 137 G protein-coupled receptors, enzymes, ion channels, transporters, and other kinases only exhibiting >50% inhibition at lymphocyte-oriented kinase (LOK) and inositol-tetrakisphosphate 1 kinase (ITPK1) at a concentration of 300 nM. APY0201 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.Formal Name: 2-[7-(4-morpholinyl)-2-(4-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]hydrazone, 3-methyl-benzaldehyde. CAS Number: 1232221-74-7. Molecular Formula: C23H23N7O. Formula Weight: 413.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 241, 323 nm. SMILES: CC1=CC=CC(/C=N/NC2=NC3=CC(C4=CC=NC=C4)=NN3C(N5CCOCC5)=C2)=C1. InChi Code: InChI=1S/C23H23N7O/c1-17-3-2-4-18(13-17)16-25-27-21-15-23(29-9-11-31-12-10-29)30-22(26-21)14-20(28-30)19-5-7-24-8-6-19/h2-8,13-16H,9-12H2,1H3,(H,26,27)/b25-16+. InChi Key: RFZQYGBLRIKROZ-PCLIKHOPSA-N.