2. MAPK/ERK Pathway Anti-infection
  3. p38 MAPK MEK Bacterial
  4. Gossypetin

Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.

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Gossypetin Chemical Structure

Gossypetin Chemical Structure

CAS No. : 489-35-0

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Based on 1 publication(s) in Google Scholar

Gossypetin Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities[1].

IC50 & Target[1]

p38 MAP kinase

 

Cellular Effect
Cell Line Type Value Description References
Huh-7 CC50
> 50 μM
Compound: 36
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
Huh-7 EC50
47 μM
Compound: 36
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
[PMID: 22445328]
MDCK CC50
283 μM
Compound: 6
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
Cytotoxicity against MDCK cells after 48 hrs by MTT assay
[PMID: 19729316]
In Vitro

Gossypetin (20-60 μM; 48 hours; KYSE30, KYSE450 and KYSE510 cells) treatment significantly inhibits anchorage-dependent esophageal cancer cell growth in dose dependent manner. Gossypetin strongly suppresses anchorage-independent cell growth in esophageal cancer cells[1].
Gossypetin (60 μM; 3 hours; KYSE30 and KYSE410 cells) treatment strongly inhibits p38 activity in a dose-dependent manner and confirms that Gossypetin directly suppresses MKK3 or MKK6 activity[1].
Gossypetin (20-40 μM; 48 hours; KYSE450 and KYSE510 cells) treatment reduces S phase and induces G2 phase cell cycle arrest in a dose-dependent manner[1].
Gossypetin (20-40 μM; 72 hours; esophageal cancer cells) treatment induces intrinsic apoptosis of esophageal cancer cells[1].

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

Gossypetin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: KYSE30, KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM, 60 μM
Incubation Time: 48 hours
Result: Anchorage-dependent esophageal cancer cell growth was significantly inhibited.

Western Blot Analysis[1]

Cell Line: KYSE30 and KYSE410 ccells
Concentration: 60 μM
Incubation Time: 3 hours
Result: p38 activity was strongly inhibited in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: KYSE450 and KYSE510 cells
Concentration: 20 μM, 40 μM
Incubation Time: 48 hours
Result: Reduced S phase and induces G2 phase cell cycle arrest in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Esophageal cancer cells
Concentration: 20 μM, 40 μM
Incubation Time: 72 hours
Result: Induced apoptosis of esophageal cancer cells.
In Vivo

Gossypetin (100 mg/kg; oral administration; 5 times per week; for 21 days; severe combined immunodeficiency (SCID) female mice) treatment significantly decreases the volume of esophageal tumor growth and without significant loss of body weight. The expression of Ki67 is significantly decreased by Gossypetin. There are no obvious morphological differences between tissues from treated or untreated mic. The phosphorylation of p38, the direct downstream protein of MKK3/6 strongly inhibited in the Gossypetin-treated group[1].

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

Animal Model: Severe combined immunodeficiency (SCID) female mice (6-9 weeks old) injection with esophageal cancer tissue[1]
Dosage: 100 mg/kg
Administration: Oral administration; 5 times per week; for 21 days
Result: Suppressed patient-derived esophageal xenograft tumor growth in an in vivo mouse model.
Molecular Weight

318.24

Formula

C15H10O8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(O)=C(OC2=C1C(O)=CC(O)=C2O)C3=CC(O)=C(C=C3)O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (392.79 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 3.1423 mL 15.7114 mL 31.4228 mL
5 mM 0.6285 mL 3.1423 mL 6.2846 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (6.54 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 (6.54 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.82%

SDS (252 KB)

COA (250 KB) RP-HPLC (99 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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 3.1423 mL 15.7114 mL 31.4228 mL 78.5571 mL
5 mM 0.6285 mL 3.1423 mL 6.2846 mL 15.7114 mL
10 mM 0.3142 mL 1.5711 mL 3.1423 mL 7.8557 mL
15 mM 0.2095 mL 1.0474 mL 2.0949 mL 5.2371 mL
20 mM 0.1571 mL 0.7856 mL 1.5711 mL 3.9279 mL
25 mM 0.1257 mL 0.6285 mL 1.2569 mL 3.1423 mL
30 mM 0.1047 mL 0.5237 mL 1.0474 mL 2.6186 mL
40 mM 0.0786 mL 0.3928 mL 0.7856 mL 1.9639 mL
50 mM 0.0628 mL 0.3142 mL 0.6285 mL 1.5711 mL
60 mM 0.0524 mL 0.2619 mL 0.5237 mL 1.3093 mL
80 mM 0.0393 mL 0.1964 mL 0.3928 mL 0.9820 mL
100 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7856 mL
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Gossypetin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gossypetin489-35-0p38 MAPKMEKBacterialMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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