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DHODH inhibitor GSK983

Chemical Structure : DHODH inhibitor GSK983

CAS No.: 827591-02-6

DHODH inhibitor GSK983 (GSK-983)

Catalog No.: PC-72538Not For Human Use, Lab Use Only.

GSK983 (GSK-983) is a potent small-molecule antiviral agent, and a potent, competitive inhibitor of dihydroorotate dehydrogenase (DHODH) with Ki of 403 nM.

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    Biological Activity

    GSK983 (GSK-983) is a potent small-molecule antiviral agent, and a potent, competitive inhibitor of dihydroorotate dehydrogenase (DHODH) with Ki of 403 nM.
    GSK983 inhibits the growth of cell lines immortalized by HTLV-1, EBV, HPV, SV40 and Ad-5, with EC50 values in the range of 10-40 nM.
    GSK983 induces either apoptosis or cytostasis at concentrations over 20 nM.
    GSK983 also inhibits cell lines immortalized by non-viral mechanisms, but has little effect on primary cells.
    GSK983 inhibited K562 cell growth with an IC50 of 21 nM, GSK983 treatment caused an accumulation of K562 cells in S phase.
    GSK983 inhibits DHODH to block virus replication and cell proliferation.
    GSK983 displayed a marked inhibitory effect on the proliferation of neuroblastoma cell lines with IC50 values from nanomoles to low micromoles.

    Physicochemical Properties

    M.Wt 325.796
    Formula C18H16ClN3O
    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

    N-[(1R)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazol-1-yl]-2-pyridinecarboxamide

    References

    1. Qi Liu, et al. Cell Chem Biol. 2020 Jun 18;27(6):668-677.e9.

    2. Robert Harvey, et al. Antiviral Res. 2009 Apr;82(1):1-11.

    3. Yajie Yu, et al. Cell Death Dis. 2021 Aug 30;12(9):821.

    4. Richard M Deans, et al. Nat Chem Biol. 2016 May;12(5):361-6.

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