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JSF-3285

Chemical Structure : JSF-3285

CAS No.:

JSF-3285 (JSF3285)

Catalog No.: PC-20079Not For Human Use, Lab Use Only.

JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.

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    Biological Activity

    JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.
    JSF-3285 demonstrated whole-cell activity versus a panel of 48 drug-sensitive and drug-resistant clinical strains comparable with its efficacy versus the H37Rv strain (MIC, 0.2 uM).
    JSF-3285 dispplayed a 30-fold increase in mouse plasma exposure compared with GSK3011724A (DG167, Catalog# PC-35948).
    JSF-3285 (100 and 200 mg/kg qd po) achieved a ~2 log10 reduction in bacterial burden in  M. tuberculosis infection CD-1 mice.
    KasA is the only essential member of three β-ketoacyl synthases encoded in the M. tuberculosis genome.
    KasA catalyzes the 2-carbon elongation of growing fatty acyl chains in the FAS-II pathway, critical to the biosynthesis of mycolic acids and, in turn, the bacterial cell wall.

    Physicochemical Properties

    M.Wt 285.34
    Formula C12H16FN3O2S
    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

    4-fluoro-N-(1-methyl-1H-indazol-6-yl)butane-1-sulfonamide

    References

    1. Inoyama D, et al. Cell Chem Biol. 2020 May 21;27(5):560-570.e10.

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