An inhibitor of PIKFYVE
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APY0201

Item No. 9001589

Technical Information
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
Purity
≥98%
A crystalline solid
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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-α in stimulated human peripheral blood mononuclear cells (PBMCs)).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hayakawa, N., Noguchi, M., Takeshita, A., et alStructure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201. Bioorg. Med. Chem. 22(11), 3021-3029 (2014).