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抑制剂/激活剂

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凋亡与自噬

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Leptomycin B 来普霉素B; CI 940; LMB

Leptomycin B (LMB, CI 940, Elactocin, Mantuamycin, NSC 364372) 是一种从链霉菌中分离的强效抗真菌抗生素，可作为核输出因子 CRM1 的特异性抑制剂。 Leptomycin B 通过共价抑制 CRM1 快速诱导癌细胞系的细胞毒性作用，IC50 值为 0.1 nM–10 nM。

货号：
TK0537
规格：

1mg

2mg
价格：
￥0.00

产品参数

CAS No.	87081-35-4
生物活性	Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
分子式	C33H48O6
分子量	540.73
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	(-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据	DMSO : 100 mg/mL (184.94 mM; Need ultrasonic) Methanol : 10 mg/mL (18.49 mM; Need ultrasonic and warming)
体内研究	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.
体外研究	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.
文献	•J Immunol. 2021 May 17;ji2001346. •Mol Med Rep. 2021 Apr 15.
纯度及产品资料	98%

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