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PIKfyve inhibitor 17

Chemical Structure : PIKfyve inhibitor 17

CAS No.: 2857982-26-2

PIKfyve inhibitor 17

Catalog No.: PC-49344Not For Human Use, Lab Use Only.

PIKfyve inhibitor 17 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) with IC50 of 4.0 nM, disrupts multiple phases of the lifecycle of β-coronaviruses (viral replication and viral entry).

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    Biological Activity

    PIKfyve inhibitor 17 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) with IC50 of 4.0 nM, disrupts multiple phases of the lifecycle of β-coronaviruses (viral replication and viral entry).
    PIKfyve inhibitor 17 displays efficacious inhibition of viral replication in the MHV-nLuc assay with IC50 of 23.5 nM.
    PIKfyve inhibitor 17 potently inhibits SARS-CoV-2 replication with IC50 of 19.5 nM in a SARS-CoV-2-nLuc assay in human epithelial A549-ACE2 cells, outperformed remdesivir.
    PIKfyve inhibitor 17 reduces uptake of His6-SARS-CoV-2 spike protein by HEK293T-ACE2 cells, inhibits uptake of lentivirus pseudotyped with the SARS-CoV-2 spike glycoprotein and impacts lysosomal homeostasis.s

    Physicochemical Properties

    M.Wt 331.423
    Formula C20H21N5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    11-(3-(Dimethylamino)prop-1-yn-1-yl)-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohepta[1,2-b]indol-2-amine

    References

    1. David H. et al. Journal of Medicinal Chemistry 2022

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