2. Metabolic Enzyme/Protease Anti-infection Apoptosis
  3. Fatty Acid Synthase (FASN) Fungal Apoptosis Antibiotic
  4. Cerulenin

Cerulenin, a potent, natural inhibitor of fatty acid synthase (FASN), is an epoxide produced by the fungus Cephalosporium caeruleus. Cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Cerulenin has antifungal and antitumor activies.

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Cerulenin 構造式

Cerulenin 構造式

CAS 番号 : 17397-89-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 278 在庫あり
Solution
10 mM * 1 mL in DMSO USD 278 在庫あり
Solid
1 mg USD 113 在庫あり
5 mg USD 238 在庫あり
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Based on 5 publication(s) in Google Scholar

Cerulenin 関連抗体

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製品説明

Cerulenin, a potent, natural inhibitor of fatty acid synthase (FASN), is an epoxide produced by the fungus Cephalosporium caeruleus. Cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Cerulenin has antifungal and antitumor activies[1][2][3][4].

IC50 & Target

Fatty acid synthase (FASN)[1]
体外実験

Cerulenin covalently binds to the catalytic site of FAS and disrupts the condensation reaction of acetyl-COA and malonyl-COA, inhibiting the biosynthesis of fatty acids and sterols in yeast. The Flavonoids quercetin and trans-Chalcone are effective against T. rubrum, with MICs of 125 and 7.5 μg/mL for the wild-type strain (MYA3108) and of 63 and 1.9 μg/mL for the ABC transporter mutant strain (ΔTruMDR2), respectively. The MICs of the Fluconazole and Cerulenin controls are 63 and 125 μg/mL for the wild-type strain and 30 and 15 μg/mL for the mutant strain, respectively[1]. To explore the underlying mechanism of Steroidogenic acute regulatory protein (StAR)’s protective effect on endothelial dysfunction model, the inhibitor of fatty acid synthase and HMG-CoA reductase, Cerulenin (5 μg/mL) and Lovastatin, are used before palmitic acid (PA) added. The mRNA expression of IL-1β, TNFα, VCAM-1 and IL-6 are reduced while NO production is recovered with inhibitor treatment[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cerulenin 関連抗体
体内実験

Cerulenin treatment of ob/ob mice has obvious effects on body weight. With 2 days of treatment, body weight in treated mice is decreased compared to a 5.7% weight gain in the controls. With prolonged (7 days) treatment, no body weight loss is observed, but body weight gain is slowed. In all groups, 60 mg/kg of Cerulenin is more effective than 30 mg/kg in inhibiting weight gain. If given daily or every other day, ATP content are increased 58.1% and 61.5% respectively by 7-day treatment of 60 mg/kg Cerulenin. Significant ATP elevation is also observed with only 2 days of treatment with 60 mg/kg Cerulenin. In contrast, 30 mg/kg Cerulenin, given either 2 or 7 days, does not show any significant effect on cellular ATP content[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

223.27

分子式

C12H17NO3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1O[C@@H]1C(CC/C=C/C/C=C/C)=O)N
Structure Classification
Initial Source

Cephalosporium caeruleus
輸送条件

Room temperature in continental US; may vary elsewhere.
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)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (447.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4789 mL 22.3944 mL 44.7888 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL
10 mM 0.4479 mL 2.2394 mL 4.4789 mL
View the 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.

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  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.20 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 DMSO 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (11.20 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 DMSO 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.
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: ≥99.0%

COA (241 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[2]

Rat aortic endothelial cells (RAECs) are isolated and cultured with minor modifications. Briefly, segments of thoracic aorta are excised from male Wistar rats (150-180 g) and immediately placed in cold PBS containing 100 U/mL Penicillin and 100 mg/mL Streptomycin. The aorta is cut into 1 millimeter wide rings after the periadventitial fat is removed. Following transferred to a T-25 cm2 flasks, the rings are cultured in Medium 199 containing 20% fetal bovine serum, 2.5 ng/mL basic fibroblast growth factors, 100U/mL Penicillin and 100 mg/mL Streptomycin. The aorta rings are placed at 37°C in a humidified atmosphere with 5% CO2 for 72-80 h without movement. All pieces of aorta rings are removed when cells migrated. Its microvascular cytological characteristics are demonstrated by CD31 and vWF staining. In experiments involving PA treatment, M199 medium supplemented with 1% bovine serum albumin is used. All experiments are performed with RAECs up to passage 4. In the experiments with inhibitor, 5 μg/mL Cerulenin (in ethonal), or 5 μM Lovastatin (in DMSO), or 3.3 μg/mL Cerulenin plus 3.3 μM Lovastatin is added in culture media 24 hours prior to PA treatment. The same volume of solvents is added at the same time as control[2].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[3]

mice[3]
Cerulenin is given to 6-8 week old male ob/ob mice in RPMI medium containing 20% DMSO intraperitoneally (i.p.). Controls are injected similarly with vehicle alone. The experimental groups (4 mice each) are as follows: A: 60 mg/kg/day Cerulenin, injected daily for 7 days; B: 60 mg/kg every other day for 7 days; C: 30 mg/kg/day for 7 days; D: 30 mg/kg every other day for 7 days; E: vehicle, daily for 7 days; F: 60 mg/kg/day Cerulenin for 2 days; G: 30 mg/kg/day Cerulenin for 2 days; H: vehicle, daily for 2 days; I: control. All animals are sacrificed on the same day under anesthesia. Blood is collected by portal vein puncture. Liver samples are snap-frozen in liquid N2 and stored at -80°C until analysis, or paraformaldehyde-fixed for histological analysis.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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
DMSO 1 mM 4.4789 mL 22.3944 mL 44.7888 mL 111.9720 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL 22.3944 mL
10 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
15 mM 0.2986 mL 1.4930 mL 2.9859 mL 7.4648 mL
20 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
25 mM 0.1792 mL 0.8958 mL 1.7916 mL 4.4789 mL
30 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
40 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
50 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
60 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
80 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
100 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
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Cerulenin Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cerulenin17397-89-6Fatty Acid Synthase (FASN)FungalApoptosisAntibioticInhibitorinhibitorinhibit

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