Leptomycin B

- Overview
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    Background
    
    Leptomycin B is a highly specific inhibitor of the export protein CRM1, with IC50 values ranging from 0.1 to 10 nM against various cancer cell lines [1].
    The exportin CRM1 is absolutely required for the nuclear export of a wide variety of cancer-related “cargo” proteins including p53, c-Abl, and FOXO-3A, cytoplasmic localization of which may result in uncontrolled growth and the onset of disease [1].
    In 15 sarcoma cell lines with varied histological backgrounds, Leptomycin B showed tumor inhibitory effects, with the average IC50 of 4.23 nM [2]. In A549 cells, Leptomycin B at the concentration of 50 nM, caused CRM1 to redistribute from the nucleus to the cytoplasm [3].
    In SiHa tumor–bearing mice, Leptomycin B (25 mg/kg, i.v., one dose per 7 days, for a total of three doses) only exhibited grow delay effects, which was consistent with the limited in vivo efficacy previously observed for Leptomycin B. In addition, Leptomycin B was also found to be relatively toxic, compared to the Leptomycin B analog [1].
    
    [1]. Mutka S C, Yang W Q, Dong S D, et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Research, 2009, 69(2): 510-517.
    [2]. Qiao Z, Kondo T. Screening of a growth inhibitor library of sarcoma cell lines to identify potent anti-cancer drugs. Journal of Electrophoresis, 2019, 63: 1-7.
    [3]. Rahmani K, Dean D A. Leptomycin B alters the subcellular distribution of CRM1 (Exportin 1). Biochem Biophys Res Commun. 2017, 488(2): 253-258.
- Properties
  - Categories
    
    Antifungal antibiotic, inhibitor of the nuclear export of proteins
    
    Alternative Name
    
    (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-((2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid
    
    CAS Number
    
    87081-35-4
    
    Molecular Formula
    
    C33H48O6
    
    Molecular Weight
    
    540.74
    
    Appearance
    
    A solution in ethanol
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥98.8 mg/mL in DMSO; ≥90.6 mg/mL in EtOH; insoluble in H2O
    
    Storage
    
    Desiccate at -20°C
    
    SMILES
    
    O[[email protected]@H]([[email protected]](C)C([[email protected]@H](/C=C(C)/C=C/C[[email protected]@H](C)/C=C(CC)\C=C\[[email protected]@H]([[email protected]](C=C1)C)OC1=O)C)=O)[[email protected]@H](C)C/C(C)=C/C(O)=O
    
    * For Research Use Only
- Reference
  - 1. Duan M, Hu F, et al. "Silencing KPNA2 inhibits IL-6-induced breast cancer exacerbation by blocking NF-κB signaling and c-Myc nuclear translocation in vitro." Life Sci. 2020;253:117736. PMID:32360571/a>

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Leptomycin B

Background

Documents

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