Genipin
Based on 22 publication(s) in Google Scholar
Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 6902-77-8
- Formula: C11H14O5
- Molecular Weight:226.23
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Storage:
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Genipin
More- Bioact Mater. 2025 Mar 10:49:207-217. [Abstract]
- Nat Commun. 2025 Jun 5;16(1):5215. [Abstract]
- Redox Biol. 2025 Jan 23:80:103511. [Abstract]
- Environ Pollut. 2021 Jun 1:278:116840. [Abstract]
- Mol Med. 2025 Oct 9;31(1):310. [Abstract]
- React Funct Polym. 2025 Sep.
- CNS Neurosci Ther. 2024 Mar;30(3):e14452. [Abstract]
- Eur J Pharmacol. 2019 Feb 15:845:56-64. [Abstract]
- Molecules. 2018 Mar 16;23(3). pii: E675. [Abstract]
- Mol Neurobiol. 2021 Aug;58(8):4134-4144. [Abstract]
- Diabetol Metab Syndr. 2025 Jul 16;17(1):267. [Abstract]
- Int J Adhes Adhes. 2025 Sep.
- Med Oncol. 2024 Jan 4;41(2):46. [Abstract]
- Epigenetics. 2018;13(3):310-317. [Abstract]
- Hum Cell. 2022 Jan;35(1):63-82. [Abstract]
- J Oral Maxillofac Surg Med Pathol. 2025 Sep 30.
- bioRxiv. 2025 Sep 21.
- bioRxiv. 2024 October 09.
- bioRxiv. 2024 July 16.
- Patent. US20230225998A1.
- J Renew Mater. 2021, 9(1), 1-16.
- Universidade de São Paulo. 2017-04-17.
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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Cell Imaging/Staining
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Histological Imaging/Staining
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Flow Cytometry
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | IC50 |
20 μg/mL
Compound: 9
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Antiviral activity against HCV infected in human Huh7 cells assessed as inhibition of viral replication after 72 hrs by NS5A staining
Antiviral activity against HCV infected in human Huh7 cells assessed as inhibition of viral replication after 72 hrs by NS5A staining
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[PMID: 19904996] |
| RAW264.7 | IC50 |
11.14 μM
Compound: 8
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Inhibition of nitric oxide production in lipopolysaccharide-activated mouse RAW264.7 cells by Griess reaction based method
Inhibition of nitric oxide production in lipopolysaccharide-activated mouse RAW264.7 cells by Griess reaction based method
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[PMID: 23305920] |
Genipin increases mitochondrial membrane potential, increased ATP levels, closed KATP channels, and stimulated insulin secretion in pancreatic islet cells. Genipin causes suppression of insulin signal transduction through hyperactivation of c-Jun N-terminal kinase (JNK) and subsequent serine phosphorylation of insulin receptor substrate-1 (IRS-1), thus impairing insulin-stimulated glucose uptake in 3T3-L1 adipocytes[1].
Genipin activates IRS-1, PI3-K, and downstream signaling pathway and increases concentrations of calcium, resulting in glucose transporter 4 (GLUT4) translocation and glucose uptake increase in C2C12 myotubes[1].
Cytochrome c content increases significantly in the cytosol of Genipin-treated FaO cells. Activation of caspase-3 and caspase-7 is ultimately responsible for Genipin-induced apoptotic process in hepatoma cells. ROS level notably increases in Hep3B cells treated with 200 μM Genipin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 6902-77-8
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Appearance Solid
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Molecular Weight 226.23
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Formula C11H14O5
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Color Off-white to light brown
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SMILES
O=C(C1=CO[C@@H](O)[C@@]2([H])[C@]1([H])CC=C2CO)OC
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Synonyms
(+)-Genipin
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Structure Classification
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
Publications (22)
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Journal Impact Factor
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Most Recent
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Bioact Mater
Engineering a stem cell-embedded bilayer hydrogel with biomimetic collagen mineralization for tendon-bone interface healing. [Abstract]2025 Mar 10:49:207-217. PMID: 40130078 -
Nat Commun
A gatekeeper sympathetic control of lacrimal tear secretion and dry eye onset through the NA-Adra1a-Ucp2 pathway. [Abstract]2025 Jun 5;16(1):5215. PMID: 40473608
Genipin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 5;16(1):5215. [Abstract]
Genipin (50 mg/kg, p.o.)-pretreated mice exhibited significantly improved tear secretion and corneal lesions.
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Redox Biol
The UCP2/PINK1/LC3b-mediated mitophagy is involved in the protection of NRG1 against myocardial ischemia/reperfusion injury. [Abstract]2025 Jan 23:80:103511. PMID: 39874927
Genipin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jan 23:80:103511. [Abstract]
UCP2 inhibitor Genipin (30 mg/kg, i.p.) significantly decreased expression levels of UCP2, LC3-Ⅱ/LC3-Ⅰ and PINK1 in the I/R myocardium by western blots.
Genipin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jan 23:80:103511. [Abstract]
Genipin (30 mg/kg, i.p.) significantly decreased expression levels of UCP2, LC3-Ⅱ/LC3-Ⅰ and PINK1 in the I/R myocardium by confocal images.
Genipin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Jan 23:80:103511. [Abstract]
The histological features of myocardial I/R injury were significantly mitigated by NRG-1 postconditioning compared with the I/R procedure and Genipin (30 mg/kg, i.p.) treatment.
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Environ Pollut
Perfluorooctane sulfonate continual exposure impairs glucose-stimulated insulin secretion via SIRT1-induced upregulation of UCP2 expression. [Abstract]2021 Jun 1:278:116840. PMID: 33689947 -
Mol Med
Dysfunctional glycolysis-UCP2-fatty acid oxidation promotes CTLA4intFOXP3int regulatory T-cell production in rheumatoid arthritis. [Abstract]2025 Oct 9;31(1):310. PMID: 41068616
Genipin purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 Oct 9;31(1):310. [Abstract]
RA-derived CD4+ T cells were treated with Genipin (25 μM) on day 3 and ROS levels were measured after 24 h.
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CNS Neurosci Ther
Rasd1 is involved in white matter injury through neuron-oligodendrocyte communication after subarachnoid hemorrhage. [Abstract]2024 Mar;30(3):e14452. PMID: 37735980 -
Eur J Pharmacol
Genipin protects against cerebral ischemia-reperfusion injury by regulating the UCP2-SIRT3 signaling pathway. [Abstract]2019 Feb 15:845:56-64. PMID: 30582911 -
Molecules
Melatonin Balance the Autophagy and Apoptosis by Regulating UCP2 in the LPS-Induced Cardiomyopathy. [Abstract]2018 Mar 16;23(3). pii: E675. PMID: 29547569
Genipin purchased from MedChemExpress. Usage Cited in: Molecules. 2018 Mar 16;23(3). pii: E675. [Abstract]
Representative image of immunobloting of UCP2 in the cultured AC16 cells under various treatments.
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Mol Neurobiol
Genipin Attenuates Tau Phosphorylation and Aβ Levels in Cellular Models of Alzheimer's Disease. [Abstract]2021 Aug;58(8):4134-4144. PMID: 33948899 -
Diabetol Metab Syndr
UCP2 inhibition exaggerates diabetic cardiomyopathy by facilitating the activation of NLRP3 and pyroptosis. [Abstract]2025 Jul 16;17(1):267. PMID: 40671041 -
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Med Oncol
Genipin inhibits proliferation of gastric cancer cells by inducing ferroptosis: an integrated study of network pharmacology and bioinformatics study. [Abstract]2024 Jan 4;41(2):46. PMID: 38175425 -
Epigenetics
Genipin normalizes depression-like behavior induced by prenatal stress through inhibiting DNMT1. [Abstract]2018;13(3):310-317. PMID: 29522357
Genipin purchased from MedChemExpress. Usage Cited in: Epigenetics. 2018;13(3):310-317. [Abstract]
Reduced BDNF protein induced by prenatal stress is normalized by the treatment of Genipin.
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Hum Cell
Serine protease HtrA2/Omi regulates adaptive mitochondrial reprogramming in the brain cortex after ischemia/reperfusion injury via UCP2-SIRT3-PGC1 axis. [Abstract]2022 Jan;35(1):63-82. PMID: 34807408 -
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (442.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4 mg/mL (17.68 mM; Need ultrasonic)
* "≥" 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.05 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.05 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 9.09 mg/mL (40.18 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
Briefly, the peptide substrate N-acetyl-Asp-Glu-Val-Asp-ρ-nitroanilide (Ac-DEVD-ρNA) is added to the cell lysates in assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM dithiothreitol, 1 mM EDTA, 10% glycerol) and incubated at 37°C. The cleavage of the substrate is monitored at 405 nm.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Kim BC, et al. Genipin-induced apoptosis in hepatoma cells is mediated by reactive oxygen species/c-Jun NH2-terminal kinase-dependent activation of mitochondrial pathway. Biochem Pharmacol. 2005 Nov 1;70(9):1398-407. [Content Brief]
[2]. Ma C, et al. Genipin stimulates glucose transport in C2C12 myotubes via IRS-1 and calcium- dependent mechanism. J Endocrinol. 2012 Dec 20. [Content Brief]
[4]. Ye D, et al. Genipin normalizes depression-like behavior induced by prenatal stress through inhibiting DNMT1. Epigenetics. 2018 Mar 9:1-22. [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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.4203 mL | 22.1014 mL | 44.2028 mL | 110.5070 mL |
| 5 mM | 0.8841 mL | 4.4203 mL | 8.8406 mL | 22.1014 mL | |
| 10 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL | 11.0507 mL | |
| 15 mM | 0.2947 mL | 1.4734 mL | 2.9469 mL | 7.3671 mL | |
| DMSO | 20 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL | 5.5254 mL |
| 25 mM | 0.1768 mL | 0.8841 mL | 1.7681 mL | 4.4203 mL | |
| 30 mM | 0.1473 mL | 0.7367 mL | 1.4734 mL | 3.6836 mL | |
| 40 mM | 0.1105 mL | 0.5525 mL | 1.1051 mL | 2.7627 mL | |
| 50 mM | 0.0884 mL | 0.4420 mL | 0.8841 mL | 2.2101 mL | |
| 60 mM | 0.0737 mL | 0.3684 mL | 0.7367 mL | 1.8418 mL | |
| 80 mM | 0.0553 mL | 0.2763 mL | 0.5525 mL | 1.3813 mL | |
| 100 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1051 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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