Leptomycin B, Free Acid **

产品名称：Leptomycin B, Free Acid
产品货号：LC  L-6100 
产品规格：1 MG
Leptomycin B (LepB) is a potent, specific inhibitor of nuclear export signal (NES)-dependent protein export from the nucleus.  Fukuda. M., et al.  "CRM1 is responsible for intracellular transport mediated by the nuclear export signal." Nature 390:  308-311 (1997).
The effect of LepB on the CRM1 (exportin 1) NES receptor results from selective alkylation by LepB of a single cysteine residue.  Kudo, N., et al.  "Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region." Proc. Natl. Acad. Sci. USA 96:  9112-9117 (1999).
LepB inhibits the nucleo-cytoplasmic translocation of the HIV Rev protein at nanomolar concentrations.  Wolff, B., et al.  "Leptomycin B is an inhibitor of nuclear export: inhibition of nucleo-cytoplasmic translocation of the human immunodeficiency virus type 1 (HIV-1) Rev protein and Rev-dependent mRNA." Chem Biol. 4:  139-147 (1997).
LepB also exhibits potent antitumor activity in vitro and in vivo, and possesses potent antimycotic and antibiotic activity.  Tunac, J.B., et al.  "Novel antitumor antibiotics, CI-940 (PD 114,720) and PD 114,721.  Taxonomy, fermentation and biological activity." J. Antibiot. 38:  460-465 (1985).
POTENCY:  LepB typically exhibits IC50 values in the 1 nM range, depending on the species, cell type, and phenomenon under study.
Our LepB is supplied in serum bottles with teflon-lined closures containing a solution in absolute ethanol (a better solvent than methanol/water; see "Solvent" below).
The 100 µg size is supplied as 185 µL of a 1 mM solution (540 µg/mL).
The 500 µg size is supplied as 925 µL of a 1 mM solution.
The 1 mg size is supplied as 1.85 mL of a 1 mM solution.
Larger quantities and higher concentrations are available - please request a quotation.
SOLVENT:  WARNING -- LEPTOMYCIN B IS UNSTABLE IN DMSO.  DO NOT USE ANY DMSO WITH LEPTOMYCIN B.  Ethanol is a better solvent for LepB than methanol for at least three reasons.  First, published information indicates that LepB is more stable in ethanol (purity unchanged after 5 months at room temperature:  US patent 4,771,070) than in methanol/water 70/30 (freezer temperatures required for storage for more than a few days:  Sigma newsletter LifeScience 2, April 2001, page 11).  Second, ethanol has a significantly higher boiling point than methanol, so ethanol solutions are expected to be less susceptible to changes in concentration due to solvent evaporation.  Third, LepB is a relatively hydrophobic compound, and may have a tendency to stick to plastic.  Being a much stronger organic solvent than methanol/water, ethanol reduces the potential loss of LepB when handled in plastic.
DILUTING LepB SOLUTIONS:  Dilutions of LepB for dose response studies should be made in an organic solvent, preferably ethanol, with only the final dilution being made into culture medium.
Storage:  Store tightly sealed at or below -20 ºC.  Solubility:  Soluble in methanol or ethanol.  Disposal:  A

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