Leptomycin B来普霉素B,87081-35-4

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Leptomycin B

CAS No. : 87081-35-4

MCE 国际站：Leptomycin B

产品活性：Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素，可阻断真核细胞周期。

研究领域：Membrane Transporter/Ion Channel  |  Anti-infection

作用靶点：CRM1  |  Fungal  |  Antibiotic

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.
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.

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.

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