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YM-201636

Cayman Chemical Item Number 13576

(CAS 371942-69-7)

YM-201636 (CAS 371942-69-7)

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Description

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).1 It reversibly impairs endosomal trafficking in NIH3T3 cells, mimicking the effect produced by depleting PIKfyve with siRNA.1 YM-201636 also blocks retroviral exit by budding from cells, apparently by interfering with the endosomal sorting complex required for transport (ESCRT) machinery.1 In adipocytes, YM-201636 also inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM).2

1 Jefferies, H.B.J., Cooke, F.T., Jat, P., et al. A selective PIKfyve inhibitor blocks PtdIns(3,5)P2 production and disrupts endomembrane transport and retroviral budding. EMBO Rep 9(2) 164-170 (2008).

2 Ikonomov, O.C., Sbrissa, D., and Shisheva, A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes. Biochem Biophys Res Commun 382 566-570 (2009).

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
Formulation A crystalline solid
Purity ≥95%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C(C1=CC=C(N)​N=C1)​NC2=CC(C3=NC4=C(OC5=C4C=CC=N5)​C(N6CCOCC6)​=N3)​=CC=C2

Background Reading

Jefferies, H.B.J., Cooke, F.T., Jat, P., et al. A selective PIKfyve inhibitor blocks PtdIns(3,5)P2 production and disrupts endomembrane transport and retroviral budding. EMBO Rep 9(2) 164-170 (2008).

Ikonomov, O.C., Sbrissa, D., and Shisheva, A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes. Biochem Biophys Res Commun 382 566-570 (2009).
Size Price Quantity Subtotal
1 mg $40.00 $0.00
5 mg $160.00 $0.00
10 mg $240.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-26. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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