来普霉素B /Leptomycin B {[allProObj[0].p_purity_real_show]}
货号：A536845同义名：
CI 940;LMB
Leptomycin B is an inhibitor of the nuclear export of proteins which acts by binding directly to and inhibiting CRM1/exportin-1. Leptomycin B inhibits the nuclear export of the HIV regulatory protein Rev and stabilizes p53, showing antiviral, antibiotic, antifunal and antitumor in vitro and in vivo.
Leptomycin B (CI 940; LMB) is a potent inhibitor of protein nuclear export, inactivating CRM1/exportin 1 through covalent modification at a cysteine residue. It has been identified as a potent antifungal antibiotic that impedes the eukaryotic cell cycle[1].
体内研究
However, Leptomycin B's in vivo tolerance is limited, with a maximum tolerated dose (MTD) of 2.5 mg/kg when administered intravenously in HCT-116 tumor-bearing mice, indicating challenges in its therapeutic application due to off-target effects. Despite its potent inhibition of CRM1, the limited in vivo efficacy suggests the need for further refinement in targeting strategies to improve tolerance and efficacy[4].
体外研究
In vitro, Leptomycin B shows high potency against various cancer cell lines, with IC50 values ranging from 0.1 to 10 nM. Specifically, it inhibits SiHa, HCT-116, and SKNSH cells with IC50 values of 0.4, 0.3, and 0.4 nM, respectively, after 72 hours of exposure[2].
Leptomycin B (LMB) (0.5 nM) has a synergistic effect on gefitinib (0-32 μM) -induced A549 and H460 cytotoxicity. Both gefitinib (0-32 μM) and Leptomycin B (0.5 nM) showed synergistic cytotoxic effects on A549 when treated for 24 and 48 h at the same time compared with gefitinib alone [3].
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