1. NF-κB Epigenetics Cell Cycle/DNA Damage MAPK/ERK Pathway Apoptosis Metabolic Enzyme/Protease
  2. NF-κB Aurora Kinase Ribosomal S6 Kinase (RSK) Apoptosis Caspase Bcl-2 Family PARP Cryptochrome
  3. Gossypin

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.

Gossypin Chemical Structure

Gossypin Chemical Structure

CAS No. : 652-78-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Gossypin:

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  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3].

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.

Cell Cycle Analysis[3]

Cell Line: HGC27 human gastric cancer cells, AGS human gastric cancer cells
Concentration: 20, 40, 60 μM (72 h), or 10, 20, 40 μM (2 weeks)
Incubation Time: (40 μM) 48 h or 72 h or 2 weeks
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.

Apoptosis Analysis[3]

Cell Line: HGC27 human gastric cancer cells
Concentration: 40, 60 μM
Incubation Time: 72 h
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).

Cell Migration Assay [3]

Cell Line: HGC27 human gastric cancer cells, AGS human gastric cancer cells
Concentration: 20, 40 μM
Incubation Time: 48 h
Result: Significantly suppressed migration.

Western Blot Analysis[1]

Cell Line: KBM-5 (chronic myeloid leukemia)
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
Incubation Time: 2.5 h (2 hours alone and then treated with TNF for 30 minutes)
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.

Western Blot Analysis[1]

Cell Line: RAW 264.7 cells, Mouse (C57BL/6J) primary bone marrow cells
Concentration: 50 μM
Incubation Time: 5 days (RAW 264.7 cells) or 3 days (primary bone marrow cells)
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

Gossypin (10-20 mg/kg; p.o.; 30 days) attenuates Isoprenaline (ISO) (HY-108353)-induced ischemic/reperfusion (I/R) in rats via alteration of oxidative stress, inflammatory reaction and gut microbiota[2].

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

Animal Model: Sprague Dawley (SD) rats (200-225 g; male; 8-10 weeks)[2]
Dosage: 10, 20 mg/kg
Administration: Oral gavage (p.o.); 30 days
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.
Molecular Weight

480.38

Formula

C21H20O13

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

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 : 250 mg/mL (520.42 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 2.0817 mL 10.4084 mL 20.8169 mL
5 mM 0.4163 mL 2.0817 mL 4.1634 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. 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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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.

  • Protocol 1

    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.
  • Protocol 2

    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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.04%

References

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
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
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