| Bioactivity | Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β. | ||||||||||||
| Invitro | Importazole specifically blocks importin-β-mediated nuclear import both in Xenopus egg extracts and cultured cells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. Importazole impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly[1]. Importazole displays an IC50 of approximately 15 μM for inhibition of NFAT-GFP import. Importazole has an IC50 of approximately 22.5 μM in HeLa cells following treatment over a 24-hour period[1]. Importazole induces a dose-and time-dependent inhibition of myeloma cells growth. And the IC50 values of importazole on RPMI 8226 and NCI-H929 after 48 hours incubation are (4.43±0.41) and (4.78±0.35) μmol/L, respectively. Treatment of RPMI 8226 and NCI-H929 cells with 8 μmol/L importazole for 24 h could inhibit NF-κB import to nucleus and reduce its DNA binding activity[2]. | ||||||||||||
| Name | Importazole | ||||||||||||
| CAS | 662163-81-7 | ||||||||||||
| Formula | C20H22N4 | ||||||||||||
| Molar Mass | 318.42 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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