Inhibitor of PIKfyve
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YM-201636

Item No. 13576

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO: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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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 reports 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(3), 566-570 (2009).

    Product Citations

    Li, Z., Mbah, N.E., Overmeyer, J.H., et al. The JNK signaling pathway plays a key role in methuosis (non-apoptotic cell death) induced by MOMIPP in glioblastoma. BMC Cancer 19(1), 77 (2019).

    Gehne, N., Lamik, A., Lehmann, M., et al. Cross-over endocytosis of claudins is mediated by interactions via their extracellular loops. PLoS One 12(8), e0182106 (2017).