YM-201636

PIKfyve is a phosphoinositide kinase (PIK) that contains a FYVE-type zinc finger domain, which binds phosphatidylinositol 3-phosphate (PI3P). PIKfyve phosphorylates PI3P to produce PI-(3,5)-P2, which is involved in cellular processes including membrane trafficking and cytoskeletal reorganization. YM-201636 is a cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM). It reversibly impairs endosomal trafficking in NIH3T3 cells, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 also blocks retroviral exit by budding from cells, apparently by interfering with the endosomal sorting complex required for transport (ESCRT) machinery. In adipocytes, YM-201636 also inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM).Formal Name: 6-amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide. CAS Number: 371942-69-7. Molecular Formula: C25H21N7O3. Formula Weight: 467.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.30 mg/ml. SMILES: O=C(C1=CC=C(N)N=C1)NC2=CC(C3=NC4=C(OC5=C4C=CC=N5)C(N6CCOCC6)=N3)=CC=C2. InChi Code: InChI=1S/C25H21N7O3/c26-19-7-6-16(14-28-19)24(33)29-17-4-1-3-15(13-17)22-30-20-18-5-2-8-27-25(18)35-21(20)23(31-22)32-9-11-34-12-10-32/h1-8,13-14H,9-12H2,(H2,26,28)(H,29,33). InChi Key: YBPIBGNBHHGLEB-UHFFFAOYSA-N.