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KSL-128114

Chemical Structure : KSL-128114

CAS No.: 2757292-12-7

KSL-128114 (KSL128114)

Catalog No.: PC-49327Not For Human Use, Lab Use Only.

KSL-128114 (KLS 128114) is a highly potent and metabolically stable peptide inhibitor that binds to the PDZ1 domain of syntenin (KD=0.3 uM), inhibits SARS-CoV-2 infection by blocking the endosomal entry of the virus.

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    Biological Activity

    KSL-128114 (KLS 128114) is a highly potent and metabolically stable peptide inhibitor that binds to the PDZ1 domain of syntenin (KD=0.3 uM), inhibits SARS-CoV-2 infection by blocking the endosomal entry of the virus.
    KSL-128114 efficiently inhibited SARS-CoV-2 viral infection in in VeroE6 cells (EC50=20 uM) with no or minor effects on cell viability.
    KSL-128114 does not bind to ACE2 in our FP-based affinity measurement, and shows 15-fold lower affinity to SNX27 (KD=5 uM).
    KSL-128114 is a novel pan-viral entry inhibitor that acts by blocking the endosomal entry pathway, also inhibits a panel of flaviviruses (dengue virus (DENV), West Nile virus 283 (WNV) and tick-born encephalitis virus (TBEV)) and an alphavirus (chikungunya virus (CHIKV)). KSL-128114 shows an inhibitory effect on primary GBM cell viability and significantly extends survival time in a patient-derived xenograft mouse model.

    Physicochemical Properties

    M.Wt 2201.628
    Formula C96H165N39O21
    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

    Ac-arg-Arg-arg-Gly-arg-Lys-lys-Arg-arg-Ser-His-Trp-Tle-Chg-Asp-Ile-OH, Ac-rRrGrKkRrSHW(Tle)(Chg)DI

    References

    1. Linda M Haugaard-Kedström, et al. J Med Chem. 2021 Feb 11;64(3):1423-1434.

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