Importazole

A cell-permeable diaminoquinazoline compound that selectively blocks importin-β-mediated nuclear import of NLS- (nuclear localization signal) bearing cargos (IC₅₀ = 15 µM against Ca⁺²-induced NFAT nuclear import in HEK293 cells) in a reversible manner without affecting transportin-dependent nuclear import of M9 signal-containing cargos or CRM1-mediated nuclear export.

A cell-permeable diaminoquinazoline compound that selectively blocks importin-β-mediated nuclear import of NLS- (nuclear localization signal) bearing cargos (IC₅₀ = 15 µM against Ca⁺²-induced NFAT nuclear import in HEK293 cells) in a reversible manner without affecting transportin-dependent nuclear import of M9 signal-containing cargos or CRM1-mediated nuclear export. IPZ affects, but not blocks, importin-β-RanGTP interaction, likely by inducing a conformational change upon direct importin-β binding. IPZ treatment impairs cellular mitosis and is cytotoxic to HeLa cells (50% and >90% killing in 24 h, respectively, with 22.5 and 60 µM IPZ).

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Soderholm, J.F., et al. 2011. ACS Chem. Biol.6, 700.

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