Leptomycin B (Synonyms: Elactocin; LMB; Mantuamycin; NSC 364372) |
Catalog No.GC10954
One-Click Copy Product Info
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Leptomycin B (LMB) est un inhibiteur de chromosome de région maintenue 1 (CRM1) qui est l'un des exporteurs de protéines nucléaires.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 87081-35-4
Sample solution is provided at 25 µL, 10mM.
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Leptomycin B (LMB) est un inhibiteur de chromosome de région maintenue 1 (CRM1) qui est l'un des exporteurs de protéines nucléaires[1]. La valeur d' IC50 de Leptomycin B est 0.1-10 nM. Leptomycin B possède les effets puissants anti-tumorals, anti-inflammatoire et neuroproctecteurs[2-3].
10-100 nM Leptomycin B(0-100 nM; 48 h) a significativement réduit la viabilité des cellules HGC-27[4]. Leptomycin B (0.5nM; 48 h) a montré un effet synergique sur la cytotoxicité gefitinib-induite dans les cellules A549[5].
Leptomycin B(30 mg/ml(100µl); i.c.v; 7 jours) empêche la formation d'oedème vasogénique induit par status epilepticus (SE), tout en préservant l'intégrité de la barrière hémato-encéphalique (BBB)[6]. Leptomycin B(10 µg/mL (20 µM), 1 µg/mL (2 µM), 100 ng/mL (200 nM), ou 10 ng/ mL (20 nM)) peut inhiber efficacement la réponse inflammatoire et l'expression de la métalloprotéinase matricelle (MMP) - 9 après l'irradiation UV-8 dans la peau de rats[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.
| Expériences cellulaires [1]: | |
Lignées cellulaires | Cellules HGC-27 |
Méthode de préparation | Les cellules ont été incubées avec 0, 1, 10, ou 100 nM leptomycin B pendant 48 h. |
Conditions de réaction | 0-100 nM; 48 h |
Domaines d'application | 10-100 nM Leptomycin B a significativement réduit la viabilité des cellules HGC-27. |
| Expériences animales [2]: | |
Modèles animaux | Rats mâles Sprague-Dawley (SD) âgés de 7 semaines |
Méthode de préparation | Les rats ont été anesthésiés et placés dans un support stéréotaxique. Un kit de perfusion cérébrale a été implanté dans le ventricule latéral droit (1 mm postérieur; 1,5 mm latéral; 3,5 mm profondeur par rapport au point de Bregma) et connecté à une pompe osmotique (1007D) contenant : (1) véhicule; (2) LMB (30 mg/ml). Les rats ont été induits à présenter les réactions épileptiques après perfusion intra-cérébroventriculaire du médicament. |
Forme de dosage | 30 mg/ml(100µl); i.c.v; 7 jours |
Domaines d'application | Leptomycin B empêche la formation d'oedème vasogénique induit par status epilepticus (SE), tout en préservant l'intégrité de la barrière hémato-encéphalique (BBB). |
References: | |
| Cas No. | 87081-35-4 | SDF | |
| Synonymes | Elactocin; LMB; Mantuamycin; NSC 364372 | ||
| Chemical Name | (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 | ||
| Formula | C33H48O6 | M.Wt | 540.74 |
| Solubility | 50mg/mL in Methanol, 50 mg/ml in Ethanol | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8493 mL | 9.2466 mL | 18.4932 mL |
| 5 mM | 369.9 μL | 1.8493 mL | 3.6986 mL |
| 10 mM | 184.9 μL | 924.7 μL | 1.8493 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solution in ethanol
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)