• Leptomycin B, EvoPure� packaged and labeled in glass vial.

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SKU: L004

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Description

Leptomycin B is the dominant member of the Leptomycin class, secondary metabolites isolated from Streptomyces spp.  It is a bioactive small molecule with antifungal and antibacterial activity.  It is a nuclear export inhibitor, targeting chromosome region maintenance 1 (CRM1), a nuclear export receptor and a protein in the nuclear export signal (NES).  It has anti-cancer activity and can modulate cancer-specific pathways.

Leptomycin B is soluble in ethanol and methanol, practically insoluble in water, and unstable in DMSO.

We also offer:

  • Leptomycin A (L020)

    CAS Number

    87081-35-4

    Molecular Formula

    C33H48O6

    Molecular Weight

    540.7

    Mechanism of Action

    Leptomycin B is a highly specific and potent inhibitor of CRM1 function. It binds irreversibly with the sulfhydryl group of a Cys residue in the cargo biding domaine of CRM1. It affects proteins c-Abl, cyclin B1, HIV-1 Rev, IκB, MPF, MAP/ERK, MDM2/p53, NF-κB/IκB7 and PKA. It inhibits the export of many RNAs (COX-2, cFOS mRNA).

    Storage Conditions

    -20°C

    Spectrum

    fungi, bacteria.

Specifications

    Appearance

    Colourless Film

    Source

    Streptomyces spp.

References

    References

    Hamamoto T. et al (1983)  Leptomycins A and B, new antifungal antibiotics. I. Taxonomy of the producing strain and their fermentation, purification and characterization.. J Antibiot. 36:639

    Hamamoto T. et al (1983)  Leptomycins A and B, new antifungal antibiotics. II. Structure elucidation.. J Antibiot. 1983, 36:646

    Jang B.C. et al (2003)  Leptomycin B, an inhibitor of the nuclear export receptor CRM1, inhibits COX-2 expression. J. Biol. Chem. 278:2773

    Kudo et al (1988)  Leptomycin B inhibition of signal-mediated nuclear export by direct binding to CRM1.

    Lu C, Shao C, Cobos E, Singh KP, Gao W (2012)  Chemotherapeutic sensitization of leptomycin B resistant lung cancer cells by pretreatment with doxorubicin. PLoS One. 7(3):e32895  PMID  22412944

    Wang Y et al (2004)  Novel leptomycins from a Streptomyces strain A92-308902: Inhibitors of the nucleo-cytoplasmic translocation of the HIV-1 regulatory protein Rev.  Helvetica 80(7):2157-2167

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