Nobiletin (Synonyms: NSC 76751, NSC 618903) |
Catalog No.GN10325
One-Click Copy Product Info
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Nobiletin is a polymethoxylated flavone extracted from citrus plants. Nobiletin has a variety of pharmacological effects, including antioxidant, anti-inflammatory, and anti-tumor properties.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 478-01-3
Sample solution is provided at 25 µL, 10mM.
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Nobiletin is a polymethoxylated flavone extracted from citrus plants[1]. Nobiletin has a variety of pharmacological effects, including antioxidant, anti-inflammatory, and anti-tumor properties[2]. Nobiletin can be used to improve metabolic syndrome and regulate lipid and blood glucose levels[3]. Nobiletin can also induce apoptosis in cancer cells, inhibit the proliferation and metastasis of tumor cells, and has potential applications in cancer therapy[4].
In vitro, Nobiletin (50–100μM) pre-treated RAW 264.7 macrophages for 16 hours, followed by stimulation with LPS (200ng/mL), significantly inhibited the expression of pro-inflammatory factors and promoted the polarization of macrophages towards the M2 phenotype by activating RORα and increasing Klf4 expression[5]. Nobiletin (2.5μM) pre-treated non-small-cell lung cancer (NSCLC) cell lines H460 and A549 for 24 hours, inhibited cell colony and sphere formation, and induced apoptosis by suppressing the activity of the WNT/β-catenin signaling pathway[6].
In vivo, Nobiletin (100mg/kg/day) was orally administered to D-galactose-induced aging C57BL/6J mice for 10 weeks. Nobiletin significantly increased mouse body weight, hindlimb muscle mass, and lean body mass, and improved skeletal muscle function. Nobiletin also improved muscle fiber size, increased the main protein components of skeletal muscle, and inhibited the production of inflammatory factors[7]. Nobiletin (100mg/kg/day) was intraperitoneally injected into C57BL/6N mice with alcohol-induced hepatic steatosis for 4 weeks. Nobiletin significantly attenuated alcohol-induced hepatic steatosis, endoplasmic reticulum stress, inflammation, and tissue damage in mice. Nobiletin reversed alcohol-induced hepatic mitochondrial dysfunction and oxidative stress[8].
References:
[1] Mileykovskaya E, Yoo SH, Dowhan W, et al. Nobiletin: Targeting the Circadian Network to Promote Bioenergetics and Healthy Aging. Biochemistry (Mosc). 2020 Dec;85(12):1554-1559.
[2] Huang J, Chang Z, Lu Q, et al. Nobiletin as an inducer of programmed cell death in cancer: a review. Apoptosis. 2022 Jun;27(5-6):297-310.
[3] Huang Q, Tian L, Zhang Y, et al. Nobiletin alleviates myocardial ischemia-reperfusion injury via ferroptosis in rats with type-2 diabetes mellitus. Biomed Pharmacother. 2023 Jul;163:114795.
[4] Moazamiyanfar R, Rezaei S, AliAshrafzadeh H, et al. Nobiletin in Cancer Therapy; Mechanisms and Therapy Perspectives. Curr Pharm Des. 2023;29(22):1713-1728.
[5] Wang SW, Lan T, Sheng H, et al. Nobiletin Alleviates Non-alcoholic Steatohepatitis in MCD-Induced Mice by Regulating Macrophage Polarization. Front Physiol. 2021 May 20;12:687744.
[6] Han SH, Han JH, Chun WJ, et al. Nobiletin Inhibits Non-Small-Cell Lung Cancer by Inactivating WNT/β-Catenin Signaling through Downregulating miR-15-5p. Evid Based Complement Alternat Med. 2021 Dec 30;2021:7782963.
[7] Wang HH, Zhang Y, Qu TQ, et al. Nobiletin Improves D-Galactose-Induced Aging Mice Skeletal Muscle Atrophy by Regulating Protein Homeostasis. Nutrients. 2023 Apr 7;15(8):1801.
[8] Lu D, Huang A, Tong X, et al. Nobiletin protects against alcohol-induced mitochondrial dysfunction and liver injury by regulating the hepatic NRF1-TFAM signaling pathway. Redox Rep. 2024 Dec;29(1):2395779.
| Cell experiment [1]: | |
Cell lines | H460 and A549 (human non-small-cell lung cancer cell lines) |
Preparation Method | Cells were cultured in DMEM supplemented with 10% FBS at 37°C, 5% CO₂. Cells were treated with Nobiletin at a concentration of 2.5μM for 24 hours. |
Reaction Conditions | 2.5μM; 24 hours |
Applications | Nobiletin significantly inhibited soft agar colony formation and increased apoptosis in NSCLC cells. Nobiletin also suppressed the invasive and migratory capacities of both A549 and H460 cells. Mechanistically, Nobiletin upregulated negative regulators of WNT/β-catenin signaling (NKD1, AXIN2, WIF1) and inhibited β-catenin and its downstream genes (c-Myc, c-Jun, Cyclin D1). Nobiletin inhibited miR-15-5p expression, which targets NKD1, AXIN2, and WIF1, thereby inactivating the WNT/β-catenin signaling pathway. |
| Animal experiment [2]: | |
Animal models | C57BL/6N wild-type mice |
Preparation Method | Mice were subjected to a Lieber-DeCarli alcohol (alcohol-fed, AF) or an isocaloric maltose dextrin control (pair-fed, PF) liquid diet for 8 weeks plus one binge. Half of the mice were supplemented with 100mg/kg/day Nobiletin via intraperitoneal injection for the final four weeks. Tissue collection occurred four hours post-gavage with ethanol (4g/kg) or isocaloric dextrin. |
Dosage form | 100mg/kg/day; i.p. |
Applications | Nobiletin administration significantly attenuated alcohol-induced hepatic steatosis, endoplasmic reticulum stress, inflammation, and tissue damage in mice. Nobiletin reversed hepatic mitochondrial dysfunction and oxidative stress in both alcohol-fed mice and acetaldehyde-treated hepatocytes. Mechanistically, Nobiletin restored the reduction of hepatic mitochondrial transcription factor A (TFAM) at both mRNA and protein levels. |
Reference: | |
| Cas No. | 478-01-3 | SDF | |
| Synonyms | NSC 76751, NSC 618903 | ||
| Chemical Name | 2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxychromen-4-one | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C(=C3OC)OC)OC)OC)OC | ||
| Formula | C21H22O8 | M.Wt | 402.39 |
| Solubility | ≥ 40.2mg/mL in DMSO | Storage | Store 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. |
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| 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 | 2.4852 mL | 12.4258 mL | 24.8515 mL |
| 5 mM | 497 μL | 2.4852 mL | 4.9703 mL |
| 10 mM | 248.5 μL | 1.2426 mL | 2.4852 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)