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GSK932121

Chemical Structure : GSK932121

CAS No.: 958457-44-8

GSK932121 (GSK-932121)

Catalog No.: PC-20294Not For Human Use, Lab Use Only.

GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.

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    Biological Activity

    GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.
    GSK932121 shows weak inhibition for cytochrome bc1 from HEK293 cells with IC50 of 400 nM (57-fold selectivity).
    GSK932121 displays potent antimalarial activity against Plasmodium falciparumin vitro (P. falciparum 3D7A, IC50=6 nM, whole cell assay).
    GSK932121 is potent against P. falciparum Pf3D70087/N9 as pyrimethamine in both HM-β2 mnull mice (ED90=0.6 mg/kg) and HM-IL2Rγnull mice (ED90=0.6 mg/kg).

    Physicochemical Properties

    M.Wt 425.79
    Formula C20H15ClF3NO4
    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

    3-chloro-6-(hydroxymethyl)-2-methyl-5-(4-(4-(trifluoromethoxy)phenoxy)phenyl)pyridin-4(1H)-one

    References

    1. Bueno JM, et al. Future Med Chem. 2012 Dec;4(18):2311-23.

    2. Capper MJ, et al. Proc Natl Acad Sci U S A. 2015 Jan 20;112(3):755-60.

    3. María Belén Jiménez-Díaz, et al. Antimicrob Agents Chemother. 2009 Oct;53(10):4533-6.

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