ボレリジン
Based on 1 publication(s) in Google Scholar
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells. Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.71%
- CAS 番号: 7184-60-3
- 分子式: C28H43NO6
- 分子量:489.64
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Borrelidin
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生物活性
製品説明
IC50 & Target
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Plasmodium |
Macrolide |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
13.97 μg/mL
Compound: Borrelidin
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Cytotoxicity against HEK293T cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 30442507] |
| HT-29 | IC50 |
0.92 μM
Compound: 1
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Growth inhibition of human HT-29 cells
Growth inhibition of human HT-29 cells
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[PMID: 25393949] |
| HUVEC | IC50 |
0.5 nM
Compound: 1, Borrelidin
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Growth inhibition in HUVEC
Growth inhibition in HUVEC
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[PMID: 16962775] |
| MDA-MB-361 | IC50 |
0.42 μM
Compound: 1
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Growth inhibition of human MDA-MB-361 cells
Growth inhibition of human MDA-MB-361 cells
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[PMID: 25393949] |
| NCI-N87 | IC50 |
0.05 μM
Compound: 1
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Growth inhibition of human NCI-N87 cells
Growth inhibition of human NCI-N87 cells
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[PMID: 25393949] |
体外実験
化学情報
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CAS 番号 7184-60-3
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性状 Solid
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分子量 489.64
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分子式 C28H43NO6
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Color White to off-white
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SMILES
O=C([C@H]1[C@H]([C@H](C/C=C/C=C(C#N)\[C@H](O)[C@@H](C)C[C@H](C)C[C@H](C)C[C@H](C)[C@@H](O)C2)OC2=O)CCC1)O
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別名
Borrelidin; Treponemycin
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Structure Classification
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Initial Source
Streptomyces rochei
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Metab
2023 Dec 5;35(12):2216-2230.e8. PMID: 37979583
溶剤 & 溶解度
体外:
Ethanol : ≥ 100 mg/mL (204.23 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Habibi D, et al. Borrelidin, a small molecule nitrile-containing macrolide inhibitor of threonyl-tRNA synthetase, is a potent inducer of apoptosis in acute lymphoblastic leukemia. Invest New Drugs. 2012 Aug;30(4):1361-70. [Content Brief]
[2]. Tsuchiya E, et al. Borrelidin inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae. J Antibiot (Tokyo). 2001 Jan;54(1):84-90. [Content Brief]
[3]. Wakabayashi T, et al. Borrelidin is an angiogenesis inhibitor; disruption of angiogenic capillary vessels in a rat aorta matrix culture model. J Antibiot (Tokyo). 1997 Aug;50(8):671-6. [Content Brief]
[4]. Otoguro K, et al. In vitro and in vivo antimalarial activities of a non-glycosidic 18-membered macrolide antibiotic, borrelidin, against drug-resistant strains of Plasmodia. J Antibiot (Tokyo). 2003 Aug;56(8):727-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol | 1 mM | 2.0423 mL | 10.2116 mL | 20.4232 mL | 51.0579 mL |
| 5 mM | 0.4085 mL | 2.0423 mL | 4.0846 mL | 10.2116 mL | |
| 10 mM | 0.2042 mL | 1.0212 mL | 2.0423 mL | 5.1058 mL | |
| 15 mM | 0.1362 mL | 0.6808 mL | 1.3615 mL | 3.4039 mL | |
| 20 mM | 0.1021 mL | 0.5106 mL | 1.0212 mL | 2.5529 mL | |
| 25 mM | 0.0817 mL | 0.4085 mL | 0.8169 mL | 2.0423 mL | |
| 30 mM | 0.0681 mL | 0.3404 mL | 0.6808 mL | 1.7019 mL | |
| 40 mM | 0.0511 mL | 0.2553 mL | 0.5106 mL | 1.2764 mL | |
| 50 mM | 0.0408 mL | 0.2042 mL | 0.4085 mL | 1.0212 mL | |
| 60 mM | 0.0340 mL | 0.1702 mL | 0.3404 mL | 0.8510 mL | |
| 80 mM | 0.0255 mL | 0.1276 mL | 0.2553 mL | 0.6382 mL | |
| 100 mM | 0.0204 mL | 0.1021 mL | 0.2042 mL | 0.5106 mL |
Borrelidin 関連分類
HY-N6742 関連分類
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