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Costunolide
別名：NSC 106404
Costunolide (NSC 106404), a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM.
CAS No. 553-21-9
文献中Selleckの製品使用例（9）
製品安全説明書
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純度：
99.99%
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Costunolide関連製品
シグナル伝達経路
Telomerase阻害剤の選択性比較
生物活性
| 製品説明 | Costunolide (NSC 106404), a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM. | ||||||
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| Targets |
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| In Vitro | ||||
| In vitro | Costunolide inhibits the growth and telomerase activity of MCF-7 and MDA-MB-231 cells in a concentration- and time-dependent manner. [1] Costunolide also inhibits the farnesylation process of human lamin-B by farnesyl–proteinttransferase (FPTase), in a dose dependent manner. Continuously treatment of Costunolide for 48 hours will significantly decrease proliferation of human tumor cells (A549, SK-OV-3, SK-MEL-2, XF498 and HCT-1) in a dose-dependent manner. [2] Costunolide induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release to the cytosol in HL-60 human leukemia cells. [3] A recent study indicates that Costunolide shows significant antifungal activity, including Trichophyton mentagrophytes, T.simlii, T.rubrum, and so on. [4] | |||
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| Kinase Assay | Telomerase activity assay | |||
| The telomerase activity is measured by the TRAP assay using the TRAPez Telomerase Detection Kit, which includes primers of a 36-bp internal control (IC) for quantifying the amplification of telomerase activity within a linear range close to 2.5 logs. For RNase treatment, 10μL of extract are incubated with 1μg of RNase at 37 °C for 20 minutes. The products of the TRAP assay are resolved by electrophoresis in a nondenaturing12% PAGE in a buffer containing 0.5 × Tris–borate EDTA and detected by autoradiograph. For quantification of TRAP products, the dried gels are exposed to Fuji Imaging Plate at room temperature. Results are corrected for background, and a standard value of 100 is given to the untreated control cell signal. Signal intensities of Costunolide-treated cells are compared to the standard and are expressed as a fraction of the maximum value of 100. [1] | ||||
| 細胞実験 | 細胞株 | MCF-7 and MDA-MB-231 cells | ||
| 濃度 | 0-100 μM | |||
| 反応時間 | 48 hours | |||
| 実験の流れ | 1) Plate 500-10,000 cells in 200 μL media per well in a 96 well plate. Leave 8 wells empty for blank controls. 2) Incubate (37 °C, 5% CO2) overnight to allow the cells to attach to the wells. 3) Add 2 μL of Costunolide dissolved in DMSO to each well. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the samples into the media. 5) Incubate (37 °C, 5% CO2) for 48 hours to allow Costunolide to take effect. 6) Make 2 mL or more of MTT solution per 96 well plate at 5 mg/mL in PBS. Do not make a stock as MTT in solution is not stable long-term. 7) Add 20 μL MTT solution to each well. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the MTT into the media. 8) Incubate (37 °C, 5% CO2) for 1-5 hours to allow the MTT to be metabolized. 9) Dump off the media. (Dry plate on paper towels to remove residue if necessary. 10) Resuspend formazan (MTT metabolic product) in 200 μL DMSO. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the formazan into the solvent. 11) Read optical density at 560 nm and subtract background at 670 nm. Optical density should be directly correlated with cell quantity. | |||
| In Vivo | ||
| In Vivo | Costunolide inhibits angiogenic response by blocking the angiogenic factor signaling pathway. In a mouse corneal micropocket assay, Costunolide reduces VEGF-stimulated neovascularization in mice. [5] | |
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| 動物実験 | 動物モデル | Hydron N containing VEGF are implanted into mouse cornea. |
| 投与量 | 100 mg/kg | |
| 投与経路 | Intraperitoneal injection once daily. | |
化学情報
| 分子量 | 232.32 | 化学式 | C15H20O2 |
| CAS No. | 553-21-9 | SDF | Download Costunolide SDFをダウンロードする |
| Smiles | CC1=CCCC(=CC2C(CC1)C(=C)C(=O)O2)C | ||
| 保管 | |||
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In vitro |
DMSO : 47 mg/mL ( (202.3 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 47 mg/mL Water : Insoluble |
モル濃度計算器 |
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in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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