Art. -Nr.: HY-16909

Leptomycin B

(Synonyms: CI 940; LMB)

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.

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Reinheit: 99.79%
CAS. Nr.: 87081-35-4
Formel: C₃₃H₄₈O₆
Molecular Weight:540.73

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Leptomycin B Chemical Structure

CAS. Nr.: 87081-35-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CRM1/exportin 1^[1]

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay	[PMID: 38105606]
HCT-116	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay	[PMID: 38105606]
HeLa	EC₅₀	0.00822 μM Compound: Leptomycin B	Inhibition of HIV1 Rev expressed in human HeLa cells co-expressing renilla luciferase reporter gene assessed as inhibition of renilla luciferase expression after 24 hrs Inhibition of HIV1 Rev expressed in human HeLa cells co-expressing renilla luciferase reporter gene assessed as inhibition of renilla luciferase expression after 24 hrs	[PMID: 18625767]
HeLa	IC₅₀	1 nM Compound: 128; LMB	Inhibition of CRM1-mediated nucleocytoplasmic transport in human HeLa cells after 90 mins by immunofluorescence assay Inhibition of CRM1-mediated nucleocytoplasmic transport in human HeLa cells after 90 mins by immunofluorescence assay	[PMID: 27996267]
MDCK	CC₅₀	>0.88 μM Compound: LMB	Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay	[PMID: 30753063]
SiHa	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay	[PMID: 38105606]
SiHa	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human SiHa cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay	[PMID: 38105606]
SK-N-SH	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 1 hrs by CellTiter Glo assay	[PMID: 38105606]
SK-N-SH	IC₅₀	0.3 nM Compound: LMB	Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human SK-N-SH cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter Glo assay	[PMID: 38105606]

In Vitro

Leptomycin B (LMB) is very potent in vitro against various cancer cell lines (IC50 values in the 0.1 to 10 nM range). Leptomycin B (LMB) inhibits SiHa, HCT-116, and SKNSH cells with IC₅₀s of 0.4, 0.3 and 0.4 nM for a 72 hour exposure, respectively^[2].
Leptomycin B (LMB) (0.5 nM) displays a synergistic effect on Gefitinib (0–32 μM)-induced cytotoxicity in A549 and H460 cell line. The simultaneous treatments of Gefitinib (0–32 μM) and Leptomycin B (0.5 nM) show synergistic cytotoxic effect on A549 as compared to Gefitinib alone at both 24 and 48 hours^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

The non-small cell lung cancer (NSCLC) cell lines A549 and H460
Concentration:

0.5 nM
Incubation Time:

24 and 48 hours
Result:

The IC₅₀ of Gefitinib at 48 hours was 32.0±2.5 μM while it was significantly reduced to 25.0±2.1 μM with the combination of 0.5 nM Leptomycin B. The significant synergistic cytotoxic effect from co-treatment of 0.5 nM Leptomycin B with Gefitinib was also confirmed in H460 cell line.

Cell Viability Assay^[3]

Cell Line:

A549
Concentration:

0.5 nM
Incubation Time:

48 hours
Result:

0.5 nM Leptomycin B plus Gefitinib or Gefitinib alone had a decreased p-EGFR(Tyr1068) expressions compared with controls.
p-Akt (Ser473) was inhibited in a dose-response manner by Gefitinib treatments, but it was enhanced by gefitinib+Leptomycin B co-treatments compared with gefitinib alone.
A549 treated by Gefitinib+Leptomycin B had a higher expression of p-Erk1/2(Thr202/Tyr204) than A549 treated by Gefitinib alone.

In Vivo

Leptomycin B (LMB) is poorly tolerated in vivo. Maximum tolerated dose (MTD) is 2.5 mg/kg for LMB (single i.v.) in HCT-116 tumor–bearing mice.The limited in vivo efficacy of Leptomycin B is due to off-target effects because our nuclear export inhibitors (NEIs) retain the potent inhibition of CRM1, but are clearly better tolerated in vivo^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 87081-35-4
Appearance <41°C Solid,>44°C Liquid
Molecular Weight 540.73
Formel C₃₃H₄₈O₆
Color White to yellow
SMILES

O=C(O)/C=C(C)/C[C@H](C)[C@@H](O)[C@H](C)C([C@H](C)/C=C(C)/C=C/C[C@@H](C)/C=C(CC)\C=C\[C@H]1[C@@H](C)C=CC(O1)=O)=O
Synonyms

CI 940; LMB
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (24)

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Journal Impact Factor

Nat Aging

Nuclear export of R-loop by the DDX1 and XPO1 complex promotes senescence-associated secretory phenotype and inflammaging. [Abstract]

2026 Jun;6(6):1208-1226. PMID: 42303864
Adv Sci (Weinh)

Lactylation of HMGB1 at K177 Drives Nuclear Export of TIAR to Promote Hypoxia-Induced Stress Granule Formation. [Abstract]

2025 Aug 11:e04896. PMID: 40788094
Adv Sci (Weinh)

Fn14 Controls the SIRT2-Mediated Deacetylation of Slug to Inhibit the Metastasis of Epithelial Ovarian Cancer. [Abstract]

2025 May 8:e2501552. PMID: 40344622
J Adv Res

Voxtalisib inhibits enterovirus 71 replication by downregulating host RAN and restoring IFN-STAT signaling. [Abstract]

2025 Jun 2:S2090-1232(25)00374-1. PMID: 40466758

Leptomycin B purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Jun 2:S2090-1232(25)00374-1. [Abstract]

Nuclear and cytoplasmic RAN, pSTAT1/2, and STAT1/2RD in RD cells treated with or without voxtalisib (37 °C, 22 h), leptomycin B (10 ng/mL; 4 h), and IFN-α (10 ng/mL).
Sci China Life Sci

3-Indolepropionic acid confers PXR-p53 binding to mitigate deoxynivalenol-induced hepatocyte apoptosis. [Abstract]

2025 Jun 20. PMID: 40553417
Emerg Microbes Infect

Inhibition of RAN attenuates influenza a virus replication and nucleoprotein nuclear export. [Abstract]

2024 Aug 1:2387910. PMID: 39087696

Leptomycin B purchased from MedChemExpress. Usage Cited in: Emerg Microbes Infect. 2024 Aug 1:2387910. [Abstract]

Cells were fixed and permeabilized at 2 h or 6 h post-infection and then immunostained for NP. Baf-A1 (100 nM) and Leptomycin (10 ng/mL) were used as nuclear import and export inhibition controls, respectively.

Leptomycin B purchased from MedChemExpress. Usage Cited in: Emerg Microbes Infect. 2024 Aug 1:2387910. [Abstract]

A549 cells treated with bepotastine (30 μM) and Leptomycin (10 ng/mL) were infected with the indicated viruses at an MOI of 10.
Cell Death Discov

CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]

2024 Oct 26;10(1):453. PMID: 39461947

Leptomycin B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]

T24 cells were treated with 1µM PD with or without 0.5nM Leptomycin B for 8 h. The subcellular localization of RB and pRB was analyzed using Western blotting.

Leptomycin B purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Oct 26;10(1):453. [Abstract]

T24 cells were treated with PD, IPZ, Leptomycin B (0.5 nM) mono- or combination therapy for 8h. Immunofluorescence staining was used to determine subcellular localization of RB and pRB. The scale bar equaled 20µm.
Cell Death Discov

MicroRNA-375 restrains the progression of lung squamous cell carcinoma by modulating the ERK pathway via UBE3A-mediated DUSP1 degradation. [Abstract]

2023 Jun 29;9(1):199. PMID: 37385985
Clin Transl Med

Selective cargo sorting in stem cell-derived small extracellular vesicles: impact on therapeutic efficacy for intervertebral disc degeneration. [Abstract]

2023 Dec;13(12):e1494. PMID: 38037469
Gastric Cancer

Nuclear export of transmembrane protein PROM2 is specially regulated by CRM1 and affects the sensitivity of ferroptosis in gastric cancer. [Abstract]

2025 Sep;28(5):837-851. PMID: 40679705
Int J Mol Sci

Lycorine Inhibits Influenza Virus Replication by Affecting Nascent Nucleoporin Nup93 Synthesis. [Abstract]

2025 Jun 3;26(11):5358. PMID: 40508167
Eur J Cell Biol

MDC1 promotes nuclear localization of Beclin-1 and supports its role in ATM pathway in response to oxidative stress. [Abstract]

2026 Apr 17;105(3):151540. PMID: 42013721
iScience

Alphaherpesvirus manipulates retinoic acid metabolism for optimal replication. [Abstract]

2024 Jun 4;27(7):110144. PMID: 38989466
J Virol

Revisiting the early event of African swine fever virus DNA replication. [Abstract]

2025 May 30:e0058425. PMID: 40444991
PLoS Genet

Nuclear p62/SQSTM1 facilitates ubiquitin-independent proteasomal degradation of BMAL1. [Abstract]

2025 Jul 10;21(7):e1011794. PMID: 40638681
Mol Med Rep

GTSE1 promotes SNAIL1 degradation by facilitating its nuclear export in hepatocellular carcin oma cells. [Abstract]

2021 Jun;23(6):454. PMID: 33880590
J Immunol

β-Arrestin 2 Regulates Inflammatory Responses against Mycobacterium tuberculosis Infection through ERK1/2 Signaling. [Abstract]

2021 Jun 1;206(11):2623-2637. PMID: 34001657
Biochem Biophys Res Commun

CRM1 mediates the nuclear export of YTHDF2. [Abstract]

2025 Jun 30:767:151899. PMID: 40315567
Biochem Biophys Res Commun

Multi-omic analysis revealed the immunological patterns and diagnostic value of exhausted T cell-derived PTTG1 in patients with psoriasis. [Abstract]

2024 Nov 19:734:150740. PMID: 39342798
Mutat Res

The oncogenic role of U2AF2/HKDC1 cascade in colorectal cancer by promoting cancer cell glycolysis and malignant phenotypes. [Abstract]

2026 Feb 6:832:111929. PMID: 41671784
bioRxiv

2026 Jan 2.
Technical University of Munich

2025.
Research Square Print

November 29th, 2022.
Research Square Print

November 29th, 2022.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (184.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8494 mL

9.2468 mL

18.4935 mL

5 mM

0.3699 mL

1.8494 mL

3.6987 mL

10 mM

0.1849 mL

0.9247 mL

1.8494 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (4.62 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. N Kudo, et al. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region. Proc Natl Acad Sci U S A. 1999 Aug 3;96(16):9112-7. [Content Brief]

[2]. Sarah C Mutka,et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]

[3]. Zhongwei Liu, et al.Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. [Content Brief]

[4]. Sarah C Mutka, et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8494 mL	9.2468 mL	18.4935 mL	46.2338 mL
	5 mM	0.3699 mL	1.8494 mL	3.6987 mL	9.2468 mL
	10 mM	0.1849 mL	0.9247 mL	1.8494 mL	4.6234 mL
	15 mM	0.1233 mL	0.6165 mL	1.2329 mL	3.0823 mL
	20 mM	0.0925 mL	0.4623 mL	0.9247 mL	2.3117 mL
	25 mM	0.0740 mL	0.3699 mL	0.7397 mL	1.8494 mL
	30 mM	0.0616 mL	0.3082 mL	0.6165 mL	1.5411 mL
	40 mM	0.0462 mL	0.2312 mL	0.4623 mL	1.1558 mL
	50 mM	0.0370 mL	0.1849 mL	0.3699 mL	0.9247 mL
	60 mM	0.0308 mL	0.1541 mL	0.3082 mL	0.7706 mL
	80 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.5779 mL
	100 mM	0.0185 mL	0.0925 mL	0.1849 mL	0.4623 mL

Leptomycin B

24 Cited Publications

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Leptomycin B

Publications Citing Use of MedChemExpress (MCE) Leptomycin B

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Leptomycin B Related Classifications

Art. -Nr.: HY-16909