Importazole - Calbiochem (C15-1303-234)

General description

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 318.42. Empirical Formula: C₂₀H₂₂N₄. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 25 . mg/mL, clear, colorless. shipped in: ambient. storage temp.: −. 20°C. SMILES string: CC(C1: CC: CC: C1)NC2: NC(: NC3: CC: CC: C32)N4CCCC4. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.