Kaempferol Estrogen/progestogen Receptor modulator

Cat.No.S2314

Kaempferol, a natural flavonol, functions as an ERRα and ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation and may also inhibit the activity of fatty acid synthase.
Kaempferol Estrogen/progestogen Receptor modulator Chemical Structure

Chemical Structure

Molecular Weight: 286.23

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 FS cells Function assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.2 μM
human HeLa cells Function assay Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM
human MV4-11 cells Cytotoxicity assay 72 h Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=3.34 μM
MDCK cells Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=4.7 μM
human MDA-kb2 cells Function assay Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=9.7 μM
B16-4A5 cells Function assay Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs, IC50=20 μM
human HL60 cells Cytotoxicity assay Cytotoxicity against human HL60 cells assessed as cell survival at 50 uM after 72 hrs by CCK8 assay
mouse 3T3L1 cells Function assay Inhibition of AMPK-mediated adipocyte differentiation in mouse 3T3L1 cells
mouse RAW264.7 cells Function assay Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 1 to 100 uM after 24 hrs by Griess method
mouse L929 cells Function assay Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment
human U87 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human U87 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
human A549 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human A549 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
human MCF7 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
MDA-MB-231 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
MDCK cells Function assay 50 μM Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in fluorescence positive cells at 50 uM immunofluorescence assay
human NCI-H2126 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human NCI-H2126 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
human SMMC7721 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
human PANC1 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human PANC1 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
human BxPC3 cells Cytotoxicity assay 5-40 μM 72 h Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 286.23 Formula

C15H10O6

Storage (From the date of receipt)
CAS No. 520-18-3 Download SDF Storage of Stock Solutions

Solubility

In vitro
Batch:

Ethanol : 28 mg/mL

DMSO : 27 mg/mL (94.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
ERRα [1]
ERRγ [1]
Topo I [2]
fatty acid synthase [3]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05073523 Completed
Healthy
Chalmers University of Technology
September 27 2021 Not Applicable

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