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Importazole Importin-β Inhibitor

Name: Importazole
Brand: Selleck Chemicals
SKU: S8446
Availability: InStock
Rating: 5 (19 reviews)

Cat.No.S8446

Importazole is a small molecule inhibitor of the transport receptor importin-β (Karyopherin beta) specifically blocking importin-β-mediated nuclear import. Importazole induces apoptosis and inhibits tumor growth.

Chemical Structure

Molecular Weight: 318.42

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Synthetic Lethality STAT TNF-alpha Ras KRas
Other Apoptosis related Inhibitors	Pitstop 2 Genipin Plumbagin 6-Gingerol Crocin Sodium propionate Colcemid Euphorbia factor L3 CWI1-2 hydrochloride Sophoridine

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (197.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (15.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	318.42	Formula	C₂₀H₂₂N₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	662163-81-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C1=CC=CC=C1)NC2=NC(=NC3=CC=CC=C32)N4CCCC4

Mechanism of Action

Targets/IC₅₀/Ki	importin-β
In vitro	Importazole is an effective inhibitor of the Ran/importin-β interaction in vitro. This compound 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. When added during mitosis, this chemical impairs the release of an importin-β cargo FRET probe and causes both predicted and novel defects in spindle assembly. It also inhibits proliferation and induces apoptosis of multiple myeloma cells by blocking the NF-κB signal pathway in vitro.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21469738/ [2] https://pubmed.ncbi.nlm.nih.gov/23668205/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Cyclin B1 / CDK1 / p-RCC1 / Cyclin D1 c-Myc		30742095

Tech Support

Handling Instructions

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