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Importazole is a cell-permeable inhibitor of importin-β, which transports cargo molecules bearing a nuclear localization signal into the nucleus.1 Importazole prevents nuclear import of GFP-tagged nuclear factor of activated T cells (NFAT-GFP) in HEK293 cells (IC50 = 15 μM), which is reversible upon importazole washout.1 Importazole does not interfere with transportin-mediated nuclear import or chromosomal maintenance 1 (CRM1)-mediated nuclear export.1 Importazole inhibits nuclear import of topoisomerase IIβ binding protein 1 (TopBP1) in Xenopus egg extracts and of NF-κB in multiple myeloma cells.2,3 It also induces defects in spindle and microtubule formation in vitro.4
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1. Importazole, a small molecule inhibitor of the transport receptor importin-
2. Importin β-
3. Effect of nuclear receptor inhibitor importazole on the proliferation and apoptosis of multiple myeloma cells. Zhonghua Xue Ye Xue Za Zhi 34(4), 323-326 (2013).
4. RanGTP and CLASP1 cooperate to position the mitotic spindle. Mol. Biol. Cell 24(16), 2506-2514 (2013).