Gossypin
Based on 1 Customer Validation
Gossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.
For research use only. We do not sell to patients.
- Purity : 98.29%
- CAS No.: 652-78-8
- Formula: C21H20O13
- Molecular Weight:480.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: NF-κB[1]
In Vitro
Gossypin (10-100 μM, 0.5-8 h and then treats with TNF for 30 minutes) inhibits NF-κB activation, leading to potentiation of apoptosis, suppression of invasion in KBM-5 cells[1].
Gossypin (50 μM, 3-5 days) inhibits RANKL-induced osteoclastogenesis in RAW 264.7 and mouse (C57BL/6J) primary bone marrow cells[1].
Gossypin (10-60 μM, 72h or 2 weeks) inhibits gastric cancer cell growth[3].
Gossypin (20-40 μM, 48 h) significantly suppresses migration in gastric cancer cell [3].
Gossypin (5-60 μM, 1-24 h) inhibits AURKA and RSK2 in JB6 cells and HGC27 cells[3].
Gossypin (40 μM, 48 h) induces G2/M phase cell cycle arrest[3].
Gossypin (40-60 μM, 72 h) increases apoptosis of gastric cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HGC27 human gastric cancer cells, AGS human gastric cancer cells
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Concentration:20, 40, 60 μM (72 h), or 10, 20, 40 μM (2 weeks)
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Incubation Time:(40 μM) 48 h or 72 h or 2 weeks
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Result:Reduced S phase and induced G2 phase cell cycle arrest.
Reduced the expression of cyclin A2, cyclin B1, and phosphorylated CDC2 proteins.
Growth of gastric cancer cells was significantly inhibited in a dose dependent manner.
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Cell Line:HGC27 human gastric cancer cells
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Concentration:40, 60 μM
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Incubation Time:72 h
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Result:Increased the number of suspended cells (dead), decreased the number of adherent cells (live).
Early and late apoptosis cells were strongly increased compared to control cells.
Increased expression of pro-apoptotic marker proteins (cleaved caspase 3, 7 and 9, cleaved PARP and cytochrome c), decreased expression of anti-apoptotic marker protein (BcL-xL).
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Cell Line:HGC27 human gastric cancer cells, AGS human gastric cancer cells
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Concentration:20, 40 μM
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Incubation Time:48 h
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Result:Significantly suppressed migration.
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Cell Line:KBM-5 (chronic myeloid leukemia)
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Concentration:0.5, 1, 2, 4, 8 h, and then treated with TNF for 30 minutes; or 2 h then treated with TNF for 16 h; or Preincubated for 30 minutes before add TNF, H2O2, PMA, LPS, IL-1β, OA, CSC
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Incubation Time:2.5 h (2 hours alone and then treated with TNF for 30 minutes)
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Result:Blocked NF-κB activation induced by tumor necrosis factor (TNF), H2O2, Phorbol myristate acetate (PMA), Lipopolysaccharides (LPS) (HY-D1056), interleukin-1β (IL-1β), okadaic acid (OA), cigarette smoke condensate (CSC).
Suppressed TNF-induced NF-κB in a dose-dependent manner.
Suppressed TNF-induced NF-κB in a time-dependent manner.
Enhanced TNF-induced apoptosis.
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Cell Line:RAW 264.7 cells, Mouse (C57BL/6J) primary bone marrow cells
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Concentration:50 μM
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Incubation Time:5 days (RAW 264.7 cells) or 3 days (primary bone marrow cells)
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Result:Decreased RANKL-induced osteoclast differentiation in RAW 264.7 cells.
50 μM concentration was sufficient to reduce osteoclastogenesis by more than 65% in RAW 264.7 cells.
Under these conditions, RAW 264.7cells remained fully viable.
Substantially decreased RANKL-induced osteoclast differentiation in primary bone marrow cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (SD) rats (200-225 g; male; 8-10 weeks)[2]
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Dosage:10, 20 mg/kg
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Administration:Oral gavage (p.o.); 30 days
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Result:Reduced the infarct size induced by Isoprenaline (ISO) (HY-108353).
Showed the boosted level of LVESP, SW, ESPVR, DP, EDPVR and suppressed level of LVEDP.
Increased the bodyweight and suppressed the heart weight and heart/body weight ratio.
Suppressed the level of triglyceride (TG), total cholesterol (TC), low-density lipoprotein (LDL), very low-density lipoprotein (VLDL) and increased the level of high-density lipoprotein (HDL).
Suppressed the level of nitric oxide synthase (iNOS) and nitric oxide (NO).
Decreased the level of MMP-2 and MMP-9.
Suppressed the level of inflammatory cytokines (TNF-α, IL-1β, IL-6) and decreased the level of NF-κB in the serum and heart tissue.
Suppressed the apoptosis of muscle fibres with edema and necrosis.
Chemical Information
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CAS No. 652-78-8
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Appearance Solid
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Molecular Weight 480.38
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Formula C21H20O13
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Color Light yellow to yellow
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SMILES
O=C1C(O)=C(C2=CC=C(O)C(O)=C2)OC3=C(O[C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)C(O)=CC(O)=C13
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 200 mg/mL (416.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (4.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
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.
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.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Ajaikumar B Kunnumakkara, et al. Gossypin, a pentahydroxy glucosyl flavone, inhibits the transforming growth factor beta-activated kinase-1-mediated NF-kappaB activation pathway, leading to potentiation of apoptosis, suppression of invasion, and abrogation of osteoclastogenesis. Blood. 2007 Jun 15;109(12):5112-21. [Content Brief]
[2]. Cheng G, et al. Cardioprotective Effect of Gossypin Against Myocardial Ischemic/Reperfusion in Rats via Alteration of Oxidative Stress, Inflammation and Gut Microbiota. J Inflamm Res. 2022 Mar 5;15:1637-1651. [Content Brief]
[3]. Wang L, et al. Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2. Phytother Res. 2019 Mar;33(3):640-650. [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. 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 |
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| DMSO | 1 mM | 2.0817 mL | 10.4084 mL | 20.8169 mL | 52.0421 mL |
| 5 mM | 0.4163 mL | 2.0817 mL | 4.1634 mL | 10.4084 mL | |
| 10 mM | 0.2082 mL | 1.0408 mL | 2.0817 mL | 5.2042 mL | |
| 15 mM | 0.1388 mL | 0.6939 mL | 1.3878 mL | 3.4695 mL | |
| 20 mM | 0.1041 mL | 0.5204 mL | 1.0408 mL | 2.6021 mL | |
| 25 mM | 0.0833 mL | 0.4163 mL | 0.8327 mL | 2.0817 mL | |
| 30 mM | 0.0694 mL | 0.3469 mL | 0.6939 mL | 1.7347 mL | |
| 40 mM | 0.0520 mL | 0.2602 mL | 0.5204 mL | 1.3011 mL | |
| 50 mM | 0.0416 mL | 0.2082 mL | 0.4163 mL | 1.0408 mL | |
| 60 mM | 0.0347 mL | 0.1735 mL | 0.3469 mL | 0.8674 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2602 mL | 0.6505 mL | |
| 100 mM | 0.0208 mL | 0.1041 mL | 0.2082 mL | 0.5204 mL |
Gossypin Related Classifications
HY-125911 Related Classifications
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