Leptomycin B (Synonyms: Elactocin; LMB; Mantuamycin; NSC 364372) |
カタログ番号GC10954
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Leptomycin B (LMB)は染色体における位置の維持1（CRM1）の阻害剤であり、核タンパク質輸出因子の1つである。
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)は染色体における位置の維持1（CRM1）の阻害剤であり、核タンパク質輸出因子の1つである。Leptomycin BのIC値は0.1-10 nMである。Leptomycin Bは強い抗腫瘍、抗炎症、神経保護の効果がある。
10-100 nMのLeptomycin B（0-100 nM；48時間）はHGC-27細胞の生存率をかなり低下する。Leptomycin B（0.5nM；48時間）はA549細胞におけるゲフィチニブ誘発性細胞毒性に相乗効果を示す。
Leptomycin B(30 mg/ml(100µl); i.c.v; 7日間)は血液脳関門（BBB）の完全性を維持を伴う状態てんかん（SE）誘導の血管原性浮腫の形成形成を防止する。Leptomycin B(10 µg/mL (20 µM), 1 µg/mL (2 µM), 100 ng/mL (200 nM)および10 ng/ mL (20 nM))は、マウスの皮膚における UV-B 照射のあとの炎症の反応とマトリックスメタロプロテイナーゼ（MMP）-9の発現を有効的に阻害できる。
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.
| 細胞実験[1]: | |
細胞株 | HGC-27 細胞株 |
準備方法 | 0, 1, 10,または100 nMのLeptomycin Bで細胞を48時間培養する。 |
反応条件 | 0-100 nM; 48 時間 |
アプリケーション | 10-100 nMのLeptomycin BはHGC-27細胞の生存率を顕著に低下させる。 |
| 動物実験 [2]: | |
動物モデル | 雄のSprague-Dawley （SD）ラット(7週齢） |
準備方法 | マウスは麻酔され、立体フレームに置かれる。脳注入キットを右心室に(後方1 mm ;側方1.5 mm; ブレグマへの深さ3.5 mm)に埋め込み、(1)賦形剤;(2)LMB(30 mg/ml)を含む浸透圧ポンプ(1007D）に繋がる。マウスは脳室内に薬を注入した後、てんかん反応が誘導される。 |
投与形態 | 30 mg/ml(100µl); i.c.v; 7日間 |
アプリケーション | Leptomycin Bは血液脳関門（BBB）の完全性を維持を伴う状態てんかん（SE）誘導の血管原性浮腫の形成形成を防止する。 |
References: | |
| Cas No. | 87081-35-4 | SDF | |
| 同義語 | 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 |
| 溶解度 | 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 | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
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.)