Leptomycin B
(Synonyms: 来普霉素B; CI 940; LMB) 目录号 : GC10954
Leptomycin B (LMB)是染色体区域维持1 (CRM1)的抑制剂,CRM1是核蛋白输出蛋白之一。
Cas No.:87081-35-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
HGC-27 cells |
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Preparation Method |
Cells were incubated with 0, 1, 10, or 100 nM of leptomycin B for 48 h. |
|
Reaction Conditions |
0-100 nM; 48 h |
|
Applications |
10-100 nM Leptomycin B significantly reduced the viability of HGC-27 cells. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley (SD) rats (7 weeks old) |
|
Preparation Method |
Mice were anesthetized and placed in a stereotaxic frame. A brain infusion kit was implanted into the right lateral ventricle (1 mm posterior; 1.5 mm lateral; 3.5 mm depth to the bregma) and connected to an osmotic pump (1007D) containing: (1) vehicle; (2) LMB (30 mg/ml). The mice were induced to have epileptic reactions after intracerebroventricular drug infusion. |
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Dosage form |
30 mg/ml(100µl); i.c.v; 7days |
|
Applications |
Leptomycin B prevents status epilepticus (SE) -induced vasogenic edema formation accompanied by preservation of blood-brain barrier (BBB) integrity. |
|
References: [1]. Zhu H, Yang Y,et,al. Leptomycin B inhibits the proliferation, migration, and invasion of cultured gastric carcinoma cells. Biosci Biotechnol Biochem. 2020 Feb;84(2):290-296. doi: 10.1080/09168451.2019.1673148. Epub 2019 Oct 16. PMID: 31619134. | |
Leptomycin B (LMB) is an inhibitor of chromosome region maintenance 1 (CRM1) that is one of the nuclear protein exporters[1]. The IC50 value of Leptomycin B is 0.1-10 nM. Leptomycin B has a potent anti-tumor, anti-inflammatory and neuroprotective effects[2-3].
10-100 nM Leptomycin B(0-100 nM; 48 h) significantly reduced the viability of HGC-27 cells[4]. Leptomycin B (0.5nM; 48 h) displayed a synergistic effect on gefitinib-induced cytotoxicity in A549 cells[5].
Leptomycin B(30 mg/ml(100µl); i.c.v; 7days) prevents status epilepticus (SE) -induced vasogenic edema formation accompanied by preservation of blood-brain barrier (BBB) integrity[6]. Leptomycin B(10 µg/mL (20 µM), 1 µg/mL (2 µM), 100 ng/mL (200 nM), or 10 ng/ mL (20 nM)) can effectively inhibit the inflammatory response and the expression of matrix metalloproteinase (MMP)-9 after UV-B irradiation in mice skin[7].
References:
[1]. Scaffidi P, Misteli T, et,al. Release of chromatin protein HMGB1 by necrotic cells triggers inflammation. Nature. 2002 Jul 11;418(6894):191-5. doi: 10.1038/nature00858. Erratum in: Nature. 2010 Sep 30;467(7315):622. PMID: 12110890.
[2]. Lu C, Shao C, et,al. Chemotherapeutic sensitization of leptomycin B resistant lung cancer cells by pretreatment with doxorubicin. PLoS One. 2012;7(3):e32895. doi: 10.1371/journal.pone.0032895. Epub 2012 Mar 7. PMID: 22412944; PMCID: PMC3296751.
[3]. Loewe R, Holnthoner W, et,al. Dimethylfumarate inhibits TNF-induced nuclear entry of NF-kappa B/p65 in human endothelial cells. J Immunol. 2002 May 1;168(9):4781-7. doi: 10.4049/jimmunol.168.9.4781. PMID: 11971029.
[4]. Zhu H, Yang Y, et,al. Leptomycin B inhibits the proliferation, migration, and invasion of cultured gastric carcinoma cells. Biosci Biotechnol Biochem. 2020 Feb;84(2):290-296. doi: 10.1080/09168451.2019.1673148. Epub 2019 Oct 16. PMID: 31619134.
[5]. Liu Z, Gao W. Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21. PMID: 28942004; PMCID: PMC5643250.
[6]. Kim DS, Min SJ, et,al. Leptomycin B ameliorates vasogenic edema formation induced by status epilepticus via inhibiting p38 MAPK/VEGF pathway. Brain Res. 2016 Nov 15;1651:27-35. doi: 10.1016/j.brainres.2016.09.023. Epub 2016 Sep 19. PMID: 27659963.
[7]. Kobayashi T, Shinkai H. Leptomycin B reduces matrix metalloproteinase-9 expression and suppresses cutaneous inflammation. J Invest Dermatol. 2005 Feb;124(2):331-7. doi: 10.1111/j.0022-202X.2004.23595.x. PMID: 15675951.
Leptomycin B (LMB)是染色体区域维持1 (CRM1)的抑制剂,CRM1是核蛋白输出蛋白之一[1]。Leptomycin B的IC50值为0.1 ~ 10 nM。Leptomycin B具有有效的抗肿瘤、抗炎和神经保护作用[2-3]。
10 ~ 100 nM Leptomycin B(0-100 nM; 48 h)显著降低HGC-27细胞活力[4]。Leptomycin B (0.5nM; 48 h)对吉非替尼Gefitinib诱导的A549细胞毒性具有协同作用[5]。
Leptomycin B(30 mg/ml(100µl); i.c.v; 7days)可以防止癫痫持续状态(SE)诱导的血管源性水肿形成,同时保持血脑屏障(BBB)的完整性[6]。Leptomycin B(10 µg/mL (20 µM), 1 µg/mL (2 µM), 100 ng/mL (200 nM), or 10 ng/ mL (20 nM))能有效抑制UV-B照射后小鼠皮肤的炎症反应和基质金属蛋白酶(MMP)-9的表达[7]。
| Cas No. | 87081-35-4 | SDF | |
| 别名 | 来普霉素B; CI 940; LMB | ||
| 化学名 | (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-((2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid | ||
| Canonical SMILES | O[C@@H]([C@H](C)C([C@@H](/C=C(C)/C=C/C[C@@H](C)/C=C(CC)\C=C\[C@@H]([C@H](C=C1)C)OC1=O)C)=O)[C@@H](C)C/C(C)=C/C(O)=O | ||
| 分子式 | C33H48O6 | 分子量 | 540.74 |
| 溶解度 | 50mg/mL in Methanol, 50 mg/ml in Ethanol | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8493 mL | 9.2466 mL | 18.4932 mL |
| 5 mM | 0.3699 mL | 1.8493 mL | 3.6986 mL |
| 10 mM | 0.1849 mL | 0.9247 mL | 1.8493 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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