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Leptomycin B

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Catalog No. T15735Cas No. 87081-35-4
Alias LMB, CI 940

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue.

Leptomycin B

Leptomycin B

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Purity: 99.04%
Catalog No. T15735Alias LMB, CI 940Cas No. 87081-35-4
Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$213In StockIn Stock
2 mg$359In StockIn Stock
5 mg$652In StockIn Stock
10 mg$928In StockIn Stock
25 mg$1,390In StockIn Stock
50 mg$1,870In StockIn Stock
100 mg$2,530-In Stock
1 mL x 10 mM (in DMSO)$297In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.04%
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Product Introduction

Leptomycin B AI Summary
Leptomycin B exhibits significant antiproliferative activity against human PC3 cells, demonstrating a fold change of 0.262 at a concentration of 10 ng/ml after 120 hours as determined by the MTT assay relative to DMSO. It effectively inhibits HIV1 Rev in human HeLa cells co-expressing renilla luciferase and firefly luciferase reporter genes, with an EC50 of 8.22 nM for renilla luciferase expression inhibition and a TC50 of 0.02 µM for firefly luciferase expression inhibition after 24 hours. Additionally, Leptomycin B inhibits CRM1-mediated nucleocytoplasmic transport in human HeLa cells with an IC50 of 1.0 nM, according to immunofluorescence assay results. This compound also exhibits antiviral activity against Influenza A virus, with an EC50 of 180.0 nM and a selectivity ratio greater than 4.0 due to a cytotoxicity CC50 greater than 880.0 nM in MDCK cells. Furthermore, Leptomycin B inhibits the fluorescently labeled PKI phi(0)Leu NES binding to human CRM1 expressed in E. coli BL21 (DE3) with an IC50 of 151.0 nM via a fluorescence polarization competition binding assay. It fully inhibits the immobilized HsCRM1-HsRanGTP-HsSPN binding to C-terminal His6-tagged and MBP-fused full-length human CRM1 expressed in E. coli SG13009 during a 20-minute pull-down assay at a concentration of 20 nmol..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue.
SynonymsLMB, CI 940
Chemical Properties
Molecular Weight540.73
FormulaC33H48O6
Cas No.87081-35-4
SmilesCC\C(\C=C\[C@H]1OC(=O)C=C[C@@H]1C)=C\[C@H](C)C\C=C\C(\C)=C\[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C\C(C)=C\C(O)=O
Relative Density.1.072 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 101 mg/mL (186.78 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.4 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8494 mL9.2468 mL18.4935 mL92.4676 mL
5 mM0.3699 mL1.8494 mL3.6987 mL18.4935 mL
10 mM0.1849 mL0.9247 mL1.8494 mL9.2468 mL
20 mM0.0925 mL0.4623 mL0.9247 mL4.6234 mL
50 mM0.0370 mL0.1849 mL0.3699 mL1.8494 mL
100 mM0.0185 mL0.0925 mL0.1849 mL0.9247 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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