Garcinol (Synonyms: Camboginol) |
Catalog No.GC13474
One-Click Copy Product Info
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Garcinol is an nonspecificity inhibitor of the histone acetyltransferases (HATs) p300 and PCAF .IC50 values are 7μM and 5μM respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 78824-30-3
Sample solution is provided at 25 µL, 10mM.
Garcinol is an nonspecificity inhibitor of the histone acetyltransferases (HATs) p300 and PCAF, IC50 values are 7μM and 5μM respectively[1-3]. It is also an nonspecificity inhibitor of potent histone deacetylase 11(HDAC11), IC50 value is 5μM[4].
Garcinol Suppresses CAL-27 cells (10μM, 24h) Proliferation and Colony Formation, inhibits Cell Cycle G1 Phase[5]. And Garcinol induces SCC-15 cells (20μM, 24h) Apoptosis[5]. Garcinol(100μM, 2h) could inhibit the elevated ROS level in H2O2 stimulation-induced Mouse Bone Marrow Mesenchymal Stem Cells(BMSCs) as well[6].
Garcinol(20mg/kg/d for 3days dissolved in 0.1% DMSO by intraperitoneal injection) could decrease inflammation and oxidative stress in cerebral ischemia-reperfusion (I/R) rats, and decreased cerebral injury of I/R rats and improved its neurological function[7]. Garcinol(20mg/kg for 5min dissolved in 0.1% DMSO and intraperitoneally injected)exhibits antithrombotic activity without impacting bleeding time under an efficacious dosage in a model of adenosine diphosphate(ADP)-induced acute pulmonary thromboembolism in mice[8].
Garcinol can prevent ischemia-reperfusion brain injury by inhibiting the TLR4/NF-ĸB signaling pathway to reduce inflammation and oxidative stress and improve nerve function[7].
References:
[1] KOPYTKO P, PIOTROWSKA K, JANISIAK J, et al. Garcinol-A Natural Histone Acetyltransferase Inhibitor and New Anti-Cancer Epigenetic Drug [J]. Int J Mol Sci, 2021, 22(6):
[2] BALASUBRAMANYAM K, ALTAF M, VARIER R A, et al. Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression [J]. J Biol Chem, 2004, 279(32): 33716-26.
[3] CAO H, AL MAMUN BHUYAN A, UMBACH A T, et al. Garcinol A Novel Inhibitor of Platelet Activation and Apoptosis [J]. Toxins, 2019, 11(7):
[4] SON S I, SU D, HO T T, et al. Garcinol Is an HDAC11 Inhibitor [J]. ACS Chem Biol, 2020, 15(11): 2866-71.
[5] ZHANG G, FU J, SU Y, et al. Opposite Effects of Garcinol on Tumor Energy Metabolism in Oral Squamous Cell Carcinoma Cells [J]. Nutrition and Cancer, 2019, 71(8): 1403-11.
[6] ZOU J, CHEN H, FAN X, et al. Garcinol prevents oxidative stress-induced bone loss and dysfunction of BMSCs through NRF2-antioxidant signaling [J]. Cell Death Discov, 2024, 10(1): 82.
[7] KANG Y, SUN Y, LI T, et al. Garcinol protects against cerebral ischemia-reperfusion injury in vivo and in vitro by inhibiting inflammation and oxidative stress [J]. Mol Cell Probes, 2020, 54(101672.
[8] HSIA C W, HUANG W C, JAYAKUMAR T, et al. Garcinol acts as a novel integrin alpha(IIb)beta(3) inhibitor in human platelets [J]. Life Sci, 2023, 326(121791.
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Cell experiment [1]: |
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Cell lines |
Mouse Bone Marrow Mesenchymal Stem Cells (BMSCs) |
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Preparation method |
The BMSCs cultured at 37°C in a humidified atmosphere with 95% air and 5% CO2. BMSCs were treated with H2O2 at 100μM for 2h to induce the intracellular oxidative stress, followed by treatment with Garcinol of Concentration gradient. |
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Reaction Conditions |
2.5μM, 5μM, 7.5μM, 10μM for 48h. |
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Applications |
Garcinol prevented oxidative stress-related BMSC damage and bone loss. |
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Animal experiment[2]: |
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Animal models |
LPS-induced male mouse calvarial osteolysis model |
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Preparation method |
Mice were injected 5mg/kg LPS and different concentration of garcinol(low‐dose:1mg/kg,high-dose:5mg/kg). Garcinol was dissolved in 5% DMSO in PBS. The mice received a subcutaneous injection over the sagittal midline suture of the calvarium under light inhalation anesthesia. |
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Dosage form |
1mg/kg, 5mg/kg: alternating days over 7‐day; subcutaneous injection. |
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Applications |
Garcinol was evidenced by marked inhibition of lipopolysaccharide‐induced bone resorption. |
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References: [1] ZOU J, CHEN H, FAN X, et al. Garcinol prevents oxidative stress-induced bone loss and dysfunction of BMSCs through NRF2-antioxidant signaling [J]. Cell Death Discov, 2024, 10(1): 82. [2] JIA Y, JIANG J, LU X, et al. Garcinol suppresses RANKL-induced osteoclastogenesis and its underlying mechanism [J]. J Cell Physiol, 2019, 234(5): 7498-509. |
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| Cas No. | 78824-30-3 | SDF | |
| Synonyms | Camboginol | ||
| Chemical Name | (1R,5R,7R)-3-(3,4-dihydroxybenzoyl)-4-hydroxy-8,8-dimethyl-5-((S)-5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl)-1,7-bis(3-methylbut-2-en-1-yl)bicyclo[3.3.1]non-3-ene-2,9-dione | ||
| Canonical SMILES | O=C1[C@](C(O)=C2C(C3=CC(O)=C(O)C=C3)=O)(C[C@H](C/C=C(C)/C)C(C)=C)C[C@@H](C/C=C(C)/C)C(C)(C)[C@@]1(C/C=C(C)/C)C2=O | ||
| Formula | C38H50O6 | M.Wt | 602.8 |
| Solubility | 20mg/mL in ethanol, 25mg/mL in DMSO, 25mg/mL in DMF | Storage | Store at -20°C,protect from light |
| 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 | 1.6589 mL | 8.2946 mL | 16.5893 mL |
| 5 mM | 331.8 μL | 1.6589 mL | 3.3179 mL |
| 10 mM | 165.9 μL | 829.5 μL | 1.6589 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: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)