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Cyanotriazole CT3

Chemical Structure : Cyanotriazole CT3

CAS No.: 2403729-27-9

Cyanotriazole CT3

Catalog No.: PC-20947Not For Human Use, Lab Use Only.

Cyanotriazole CT3 is a potent, selective, irreversible inhibitor of trypanosomal topoisomerase II, shows potent trypanocidal activity both in vitro and in vivo.

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    Biological Activity

    Cyanotriazole CT3 is a potent, selective, irreversible inhibitor of trypanosomal topoisomerase II, shows potent trypanocidal activity both in vitro and in vivo.
    Cyanotriazole CT3 is a potent growth inhibitor of a panel of kinetoplastid parasites, which includes T. cruzi and L. donovani (EC50, 78 and 134 nM), but has no activity against a range of nontrypanosomatid microbial pathogens.
    Cyanotriazole CT3 (30 mg/kg) is efficacious against trypanosomatid parasites in vivo.
    Cyanotriazole CT3-treated parasites showes defects in nuclear DNA replication, exhibited up-regulated DNA damage response.
    Cyanotriazole CT3 selectively inhibits the DNA relaxation activity of trypanosome TopoII by stabilizing the dsDNA:enzyme complex, interacts covalently with C477 and bind at the DNA cleavage site.

    Physicochemical Properties

    M.Wt 416.34
    Formula C19H12F4N6O
    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

    1-(2-(5-(5-fluoro-2-(trifluoromethyl)pyridin-3-yl)isoindolin-2-yl)-2-oxoethyl)-1H-1,2,4-triazole-3-carbonitrile

    References

    1. Srinivasa P S Rao, et al. Science. 2023 Jun 30;380(6652):1349-1356.

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