Chemical Property of N-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-aMine
Chemical Property:
- Boiling Point:516.8±42.0 °C(Predicted)
- PKA:7.27±0.59(Predicted)
- PSA：41.05000
- Density:1?+-.0.06 g/cm3(Predicted)
- LogP:4.54110
- Storage Temp.:2-8°C
- Solubility.:DMSO: >5mg/mL
- Purity/Quality:
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99%, *data from raw suppliers
Importazole *data from reagent suppliers
Safty Information:
- Pictogram(s):
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- MSDS Files:
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Useful:
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Description
Importazole is a cell-permeable inhibitor of importin-β, which transports cargo molecules bearing a nuclear localization signal into the nucleus. 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. Importazole does not interfere with transportin-mediated nuclear import or chromosomal maintenance 1 (CRM1)-mediated nuclear export. Importazole inhibits nuclear import of topoisomerase IIβ binding protein 1 (TopBP1) in Xenopus egg extracts and of NF-κB in multiple myeloma cells. It also induces defects in spindle and microtubule formation in vitro.
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Uses
Importazole has been used:to inhibit importin-β and to elucidate the mechanism of enhanced nuclear localization of heat shock protein 70 (HSP70) by vaccinia-related kinase 3 (VRK3)to treat COS?7 cells transfected with the expressing vectors of WT HNF4α , S78A, and S78D to study its effectas a KPNB inhibitor to determine whether CREB-regulated co-activator 1 (CRTC1) would be escorted into the nucleus by the classical nuclear localizing sequence (NLS)- dependent machineryas a functional inhibitor of Importin β in embryo treatmentas an?importin?inhibitor to treat the transfected H1299 cells to block nuclear translocation of phosphorylated p53-RS Importazole is an importin-β inhibitor.
