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SGC-PIKFYVE-1

Chemical Structure : SGC-PIKFYVE-1

CAS No.: 2857982-26-2

SGC-PIKFYVE-1 (PIKfyve inhibitor 17)

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

SGC-PIKFYVE-1 is a potent, selective and cell-active chemical probe inhibitor of PIKfyve with IC50 of 4.0 nM in NanoBRET assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    SGC-PIKFYVE-1 is a potent, selective and cell-active chemical probe inhibitor of PIKfyve with IC50 of 4.0 nM in NanoBRET assays.
    SGC-PIKFYVE-1 inhibits viral replication in the MHV-nLuc assay with IC50 of 23.5 nM, also is a potent inhibitor of SARS-CoV-2 replication, outperformed remdesivir (IC50=86.4 nM).
    SGC-PIKFYVE-1 demonstrates good kinome-wide selectivity, binding with PoC < 10 to nine or fewer WT human kinases at 1 μM.
    SGC-PIKFYVE-1 reduces uptake of His6-SARS-CoV-2 spike protein by HEK293T-ACE2 cells, impacts lysosomal homeostasis.
    SGC-PIKFYVE-1 disrupts multiple phases of the lifecycle of β-coronaviruses: viral replication and viral entry.
    SGC-PIKFYVE-1 (10 µM) also inhibits voltage-gated sodium currents through the inhibition of Nav1.7 and Nav1.8 channels, without affecting voltage-gated calcium or potassium currents in sensory neurons.
    SGC-PIKFYVE-1 (30 mg/kg) alleviated mechanical and cold sensitivity induced by neuropathic or inflammatory pain in both male and female mice, without causing motor impairments.

    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. Drewry DH, et al. J Med Chem. 2022 Oct 13;65(19):12860-12882.
    2. Rodríguez-Palma EJ, et al. Neurobiol Pain. 2024 Nov 29;17:100174. 

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