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TPP8

Chemical Structure : TPP8

CAS No.: 1581683-17-1

TPP8 (Bacterial DNA Gyrase inhibitor)

Catalog No.: PC-49326Not For Human Use, Lab Use Only.

TPP8 is a small molecule antibacterial inhibiting the ATPase of DNA gyrase with IC50 of 0.3 uM, binds and inhibits the ATPase domain of the gyrase B subunit, shows activity against M. abscessus strains with MIC of 0.04-0.2 uM.

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    Biological Activity

    TPP8 is a small molecule antibacterial inhibiting the ATPase of DNA gyrase with IC50 of 0.3 uM, binds and inhibits the ATPase domain of the gyrase B subunit, shows activity against M. abscessus strains with MIC of 0.04-0.2 uM.
    TPP8 exhibited a markedly higher potency than SPR719 or moxifloxacin.
    TPP8 inhibited DNA supercoiling activity of recombinant M. abscessus enzyme.
    TPP8 demonstrated proof-of-concept activity against M. abscessus ex vivo and in vivo in macrophage and mouse infection studies.

    Physicochemical Properties

    M.Wt 482.496
    Formula C23H24F2N8O2
    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

    (S)-1-(5-((4-((R)-5-amino-2-azaspiro[3.3]heptan-2-yl)-5,6-difluoro-8-(methylamino)-9H-pyrimido[4,5-b]indol-2-yl)oxy)pyrimidin-2-yl)ethan-1-ol

    References

    1. Abdeldjalil Madani, et al. Antimicrob Agents Chemother. 2022 Sep 20;66(9):e0066922.

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