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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. 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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 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 |
| InChI key | HKGJEZIGDHFJFL-UHFFFAOYSA-N |
| 长度(mm) | |
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