A cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM); reversibly impairs endosomal trafficking in NIH3T3 cells and blocks retroviral exit by budding from cells; inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM) in adipocytes

YM-201636 – 10 mg

Brand:
Cayman
CAS:
371942-69-7
Storage:
-20
UN-No:
Non-Hazardous - /

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).{18015} It reversibly impairs endosomal trafficking in NIH3T3 cells, mimicking the effect produced by depleting PIKfyve with siRNA.{18015} YM-201636 also blocks retroviral exit by budding from cells, apparently by interfering with the endosomal sorting complex required for transport (ESCRT) machinery.{18015} In adipocytes, YM-201636 also inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM).{18016}  

 

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Description

A cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM); reversibly impairs endosomal trafficking in NIH3T3 cells and blocks retroviral exit by budding from cells; inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM) in adipocytes

Formal name: 6-amino-N-[3-[4-(4-morpholinyl)pyrido[3′,2′:4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide

Synonyms: 

Molecular weight: 467.5

CAS: 371942-69-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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