Importazole


Catalog No. Size PriceQuantity
M12353-2 2mg solid $100
M12353-10 10mg solid $300

Description

Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.

Product information

CAS Number: 662163-81-7

Molecular Weight: 318.42

Formula: C20H22N4

Chemical Name: N-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine

Smiles: CC(NC1=NC(=NC2=CC=CC=C21)N1CCCC1)C1C=CC=CC=1

InChiKey: HKGJEZIGDHFJFL-UHFFFAOYSA-N

InChi: InChI=1S/C20H22N4/c1-15(16-9-3-2-4-10-16)21-19-17-11-5-6-12-18(17)22-20(23-19)24-13-7-8-14-24/h2-6,9-12,15H,7-8,13-14H2,1H3,(H,21,22,23)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 33 mg/mL (103.64 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. 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. 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.

References:

  1. Soderholm JF, et al. Importazole, a small molecule inhibitor of the transport receptor importin-β. ACS Chem Biol. 2011 Jul 15;6(7):700-8.
  2. Yan WQ, et al. Effect of nuclear receptor inhibitor importazole on the proliferation and apoptosis of multiple myeloma cells. Zhonghua Xue Ye Xue Za Zhi. 2013 Apr;34(4):323-6.

Products are for research use only. Not for human use.

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