2. Metabolic Enzyme/Protease Stem Cell/Wnt Neuronal Signaling Immunology/Inflammation NF-κB Anti-infection TGF-beta/Smad Protein Tyrosine Kinase/RTK
  3. Glycosidase Notch Toll-like Receptor (TLR) NF-κB Mucin Reactive Oxygen Species (ROS) Bacterial TGF-beta/Smad Anaplastic lymphoma kinase (ALK)
  4. Kaempferol 3-O-gentiobioside

Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma. It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer.

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Kaempferol 3-O-gentiobioside

Kaempferol 3-O-gentiobioside Chemical Structure

CAS No. : 22149-35-5

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Kaempferol 3-O-gentiobioside Related Antibodies

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Description

Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma. It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer[1][2][3][4].

In Vitro

Kaempferol 3-O-gentiobioside binds to recombinant human NOTCH1 with a Kd value of 57 µM[1].
Kaempferol 3-O-gentiobioside (0-100 µM; 24-72 h) exhibits dose- and time-dependent cytotoxicity in 16HBE cells, while concentrations of 5, 25 and 50 µM show no cytotoxicity at 24 h[1].
Kaempferol 3-O-gentiobioside (0-50 µM; 1 h pretreatment, followed by 24 h IL-13 stimulation) dose-dependently reduces nitrite production, decreases ROS levels, inhibits the secretion of IgE, TNF-α, histamine, IL-1β, IL-6 and IL-8, and suppresses the mRNA and protein expression of MUC5AC in IL-13-stimulated 16HBE cells[1].
Kaempferol 3-O-gentiobioside (0-50 µM; administered 24 h after IL-13 stimulation) dose-dependently inhibits IL-13-induced activation of the NOTCH pathway, including downregulating the expression of NOTCH1, NOTCH2, NOTCH3 and DLL4 in 16HBE cells, while also reducing the basal expression levels of these components[1].
Kaempferol 3-O-gentiobioside (0-50 µM; administered 24 h after IL-13 stimulation) inhibits IL-13-induced activation of the TLR4/NF-κB/NLRP3 pathway in 16HBE cells, including downregulating the expression of TLR4, NLRP3, p-IκBα and p-P65, as well as suppressing the activation of NF-κB/P65[1].
Kaempferol 3-O-gentiobioside moderately inhibits yeast α-glucosidase (derived from Saccharomyces cerevisiae) with an IC50 value of 50 μM[2].
Kaempferol 3-O-gentiobioside (0-100 μM; 24 h) exhibits concentration-dependent antibacterial activity against methicillin-resistant *Staphylococcus aureus* (ATCC 43300), with an MIC of 8.3 μM and an MBC of 16.5 μM, and inhibits biofilm formation[3].
Kaempferol 3-O-gentiobioside (pretreated for 2 h, followed by stimulation with TGFβ1 for 24 h) potently inhibits the TGF-β/ALK5/Smad signaling pathway in HACAT cells, with an IC50 of 2.589 μM[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 2 h) inhibits the TGF-β/ALK5/Smad signaling pathway in MDA-MB-231, AGS and SKOV3IP1 cells in a concentration-dependent manner by reducing the levels of p-Smad2 and Smad4[4].
Kaempferol 3-O-gentiobioside (24 h) inhibits the proliferation of MDA-MB-231, AGS and SKOV3IP1 cells, with IC50 values of 6.83 μM, 9.6 μM and 11.12 μM, respectively[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 24 h) reduces the colony-forming ability of MDA-MB-231, AGS and SKOV3IP1 cells in a concentration-dependent manner[4].
Kaempferol 3-O-gentiobioside (2 μM; 24 h) inhibits TGFβ-induced migration and invasion of MDA-MB-231, AGS and SKOV3IP1 cells[4].
Kaempferol 3-O-gentiobioside (0-4 μM; 2 h) concentration-dependently reverses TGFβ-induced epithelial-mesenchymal transition (EMT) in MDA-MB-231, AGS and SKOV3IP1 cells by restoring E-cadherin levels and reducing the levels of N-cadherin, vimentin and snail transcription factor (snail)[4].

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

Kaempferol 3-O-gentiobioside Related Antibodies

Cell Viability Assay[1]

Cell Line: human bronchial epithelial 16HBE cells
Concentration: 0,5, 25, 50, 100 µM
Incubation Time: 24 h; 48 h; 72 h
Result: Did not cause significant cytotoxicity at 50 µM at 24 h, while 100 µM significantly reduced cell viability.
Reduced cell viability in a dose-dependent manner at 48 h and 72 h.

ELISA Assay[1]

Cell Line: IL-13-stimulated human bronchial epithelial 16HBE cells
Concentration: 0, 5, 25, 50 µM
Incubation Time: treatment after 24 h IL-13 stimulation
Result: Reduced IL-13-induced levels of IgE, TNF-α, histamine, IL-1β, IL-6, and IL-8 in a dose-dependent manner, with the most significant reductions seen at 50 µM.

Western Blot Analysis[4]

Cell Line: MDA-MB-231 (breast cancer), AGS (gastric cancer), SKOV3IP1 (ovarian cancer) cells
Concentration: 0, 0.5, 1, 2, 4 μM
Incubation Time: 2 hr pretreatment, followed by 24 hr TGFβ stimulation
Result: Concentration-dependently suppressed TGF-β-induced phosphorylation of Smad2 and downregulated Smad4 expression in all three cell lines, with no obvious effect on total Smad2 expression.

Immunofluorescence[4]

Cell Line: MDA-MB-231, AGS, SKOV3IP1 cells
Concentration: 2 μM
Incubation Time: 2 hr pretreatment, followed by 24 hr TGFβ stimulation
Result: Significantly reduced the fluorescence intensity of p-Smad2 and Smad4 in all three cell lines compared to DMSO-treated controls.

Western Blot Analysis[4]

Cell Line: SKOV3IP1 cells
Concentration: 2 μM
Incubation Time: 2 h pretreatment, followed by 24 hr TGFβ stimulation
Result: Failed to further reduce TGFβ-induced p-Smad2 expression compared to ALK5 knockdown alone.
Left total Smad2 expression unchanged across groups.

Cell Migration Assay[4]

Cell Line: SKOV3IP1 cells
Concentration: 2 μM
Incubation Time: 30 hr incubation with TGFβ stimulation
Result: Showed inhibitory effects on TGFβ-induced wound closure similar to ALK5 knockdown.
Produced no significant additional reduction in wound closure when co-treated with ALK5 siRNA compared to ALK5 siRNA alone.

Western Blot Analysis[4]

Cell Line: MDA-MB-231, AGS, SKOV3IP1 cells
Concentration: 0.5-4 μM
Incubation Time: 2 hr pretreatment, followed by 24 hr TGFβ stimulation
Result: Restored TGFβ-reduced E-cadherin expression and downregulated TGFβ-increased N-cadherin, vimentin, and snail expression in a concentration-dependent manner across all three cell lines.

Immunofluorescence[4]

Cell Line: MDA-MB-231, AGS, SKOV3IP1 cells
Concentration: 4 μM
Incubation Time: 2 hr pretreatment, followed by 24 hr TGFβ stimulation
Result: Increased TGFβ-reduced E-cadherin fluorescence intensity and decreased TGFβ-increased N-cadherin and snail fluorescence intensity in all three cell lines.
Reduced TGFβ-induced nuclear localization of snail.
In Vivo

Kaempferol 3-O-gentiobioside (10-40 mg/kg; p.o.; once daily; for 7 consecutive days) dose-dependently alleviates airway inflammation and mucus hypersecretion in OVA (HY-W250978)-induced allergic asthma mice[1].
Kaempferol 3-O-gentiobioside (40 mg/kg; p.o.; once daily; for 30 consecutive days) reduces the average volume of ovarian cancer xenograft tumors to 584 mm3[4].

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

Animal Model: BALB/c (female, 4 weeks old, 18-20 g, OVA-induced allergic asthma model)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: p.o.; daily; 7 days
Result: Lowered lung inflammation score to ~2.5 (10 mg/kg), ~1.5 (20 mg/kg), and ~1.2 (40 mg/kg) compared to OVA-only group score of ~3.7.
Reduced lung tissue levels of TNF-α to ~120 pg/mL, histamine to ~1200 ng/mL, IL-1β to ~950 pg/mL, IL-6 to ~1200 pg/mL, IL-8 to ~1200 pg/mL at 40 mg/kg dose compared to OVA-only group levels of ~550 pg/mL, ~1800 ng/mL, ~1500 pg/mL, ~1600 pg/mL, ~1800 pg/mL respectively.
Lowered PAS-positive area percentage to ~14% (10 mg/kg), ~9% (20 mg/kg), ~6% (40 mg/kg) compared to OVA-only group ~23%.
Lowered MUC5AC mRNA relative level to ~1.2 (10 mg/kg), ~0.8 (20 mg/kg), ~0.6 (40 mg/kg) compared to OVA-only group ~2.4.
Lowered MUC5AC protein concentration to ~350 pg/mL (10 mg/kg), ~300 pg/mL (20 mg/kg), ~250 pg/mL (40 mg/kg) compared to OVA-only group ~550 pg/mL.
Lowered NOTCH1/β-actin ratio to ~0.45, NOTCH2/β-actin ratio to ~0.1, NOTCH3/β-actin ratio to ~0.45, DLL4/β-actin ratio to ~0.6 at 40 mg/kg dose compared to OVA-only group ratios of ~0.8, ~0.9, ~0.9, ~1.2 respectively.
Animal Model: BALB/c nude (female, 5 weeks old, 16 g)[4]
Dosage: 40 mg/kg
Administration: p.o.; daily; 30 days
Result: Reduced mean tumor volume to 584 mm3 on day 30 (vs.
1210 mm3 in vehicle control).
Significantly lowered mean tumor weight relative to vehicle control.
Downregulated expression of p-Smad2 and Smad4 in tumor tissue compared to vehicle control.
Showed no significant difference in mouse body weight vs.
vehicle control.
Caused no detectable abnormalities in heart, liver, spleen, and kidney via H&E staining.
Molecular Weight

610.52

Formula

C27H30O16
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1C(O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)O2)O)O)O)=C(C4=CC=C(O)C=C4)OC5=CC(O)=CC(O)=C15
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (81.90 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 1.6379 mL 8.1897 mL 16.3795 mL
5 mM 0.3276 mL 1.6379 mL 3.2759 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 (protect from light). 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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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.09 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.
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, . 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 (protect from light)

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
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 (protect from light). 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 1.6379 mL 8.1897 mL 16.3795 mL 40.9487 mL
5 mM 0.3276 mL 1.6379 mL 3.2759 mL 8.1897 mL
10 mM 0.1638 mL 0.8190 mL 1.6379 mL 4.0949 mL
15 mM 0.1092 mL 0.5460 mL 1.0920 mL 2.7299 mL
20 mM 0.0819 mL 0.4095 mL 0.8190 mL 2.0474 mL
25 mM 0.0655 mL 0.3276 mL 0.6552 mL 1.6379 mL
30 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3650 mL
40 mM 0.0409 mL 0.2047 mL 0.4095 mL 1.0237 mL
50 mM 0.0328 mL 0.1638 mL 0.3276 mL 0.8190 mL
60 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6825 mL
80 mM 0.0205 mL 0.1024 mL 0.2047 mL 0.5119 mL
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Kaempferol 3-O-gentiobioside Related Classifications

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    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:

Kaempferol 3-O-gentiobioside22149-35-5GlycosidaseNotchToll-like Receptor (TLR)NF-κBMucinReactive Oxygen Species (ROS)BacterialTGF-beta/SmadAnaplastic lymphoma kinase (ALK)Nuclear factor-κBNuclear factor-kappaBTransforming growth factor betaAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK5TGF-β/ALK5/Smad signalingNLRP3MUC5ACMRSANOTCH signalingyeast α-glucosidaseTLR4NOTCH1flavonoidallergic asthmadiabetesMRSA infectionbreast cancergastric cancerovarian cancerInhibitorinhibitorinhibit

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