5-methoxyflavone

Alias: 5-Methoxyflavone
Cat No.:V3120 Purity: ≥98%
5-methoxyflavone, a flavonoid analog, is a novel DNA polymerase-ß inhibitor and neuroprotective agent against ß-amyloid toxicity.
5-methoxyflavone Chemical Structure CAS No.: 42079-78-7
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

5-methoxyflavone, a flavonoid analog, is a novel DNA polymerase-ß inhibitor and neuroprotective agent against ß-amyloid toxicity. 5-Methoxyflavone was confirmed to be an inhibitor of DNA pol-β activity using cultured primary neurons, a valuable model for examining the neuroprotective effects of putative DNA pol-β inhibitors because treatment with Aβ causes DNA replication and cell death in these neurons. 5-methoxyflavone decreased the number of S-phase neurons and the subsequent apoptotic death induced by Aβ, which is consistent with the inhibition of DNA pol-β. 5-Methoxyflavone is the first flavonoid compound that, as opposed to having broad antioxidant and anti-inflammatory effects, is able to stop neurodegeneration through a specific molecular mechanism.

Biological Activity I Assay Protocols (From Reference)
Targets
DNA polymerase β
ln Vitro

In vitro activity: 5-Methoxyflavone (compound 1) has been identified as a potential compound that can inhibit DNA pol-β in multiple instances and prevent the initiation of the cell cycle and subsequent neuronal apoptosis in primary neuronal cultures challenged with Aβ. On 92TAg cells, 5-methoxyflavone (10–30 μM) can greatly increase the toxicity of MMS. 5-Polymerase activity on a gapped substrate is significantly reduced by 1- or 10-methoxyflavone[1]. 5-Methoxyflavone (5-MF, 0-100 μg/mL) causes the proapoptotic protein BAX to increase and the antiapoptotic proteins cFLIP and Mcl-1 to decrease over time. 5-MF induces TRAIL-R1 (DR4) and TRAIL-R2 (DR5) in a manner that is dependent on time[2].

ln Vivo
5-Methoxyflavone (100, 150 mg/kg, i.p) dramatically reduces the amount of time it takes to lose the righting reflex. 5. A notable and dose-dependent decrease in spontaneous locomotor activity is shown by methylflavone (50, 100, and 150 mg/kg, i.p.). 5. The rearing response is decreased by methylflavone (50, 100 mg/kg, i.p.). 5-The grooming response was totally eliminated by methylflavone (100, 125, and 150 mg/kg, i.p. ), just like in animals treated with diazepam[3].
Enzyme Assay
Human DNA Pol-β Assay [1]
DNA pol-β inhibition was evaluated with a specific DNA pol-β assay kit. The assay was carried out strictly following the manufacturer’s instructions. Briefly, a reaction mixture containing a gapped DNA template, dNTPs (both supplied with the kit), and DNA pol-β was incubated for 30 min at RT with or without the compound to be tested. The formation of repaired duplexes, which, unlike gapped DNA, selectively incorporate a fluorescent dye in the presence of Reagent U (both supplied by the kit) was determined by measuring at 535 nm with the excitation wavelength at 485 nm in a fluorimeter. OA (50 μM) was used as a positive control for inhibition. Activity was evaluated as fluorescent signal to no-enzyme-background ratio.
Cell Assay
The MTT assay is used to assess the cell viability after treating MOLT-4, U937, or PBMC cells with DMF, TMF, PMF, 5-MF, or 2'-MF at different concentrations for 24 hours.
Animal Protocol


References

[1]. Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity. J Nat Prod. 2015 Nov 25;78(11):2704-11.

[2]. Sedative-hypnotic like effect of 5-methoxyflavone in mice and investigation on possible mechanisms by in vivo and in silico methods. Biomed Pharmacother. 2018 Dec;108:85-94.

[3]. Methoxyflavone derivatives modulate the effect of TRAIL-induced apoptosis in human leukemic cell lines. J Hematol Oncol. 2011 Dec 21;4:52.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H12O3
Molecular Weight
252.26
Exact Mass
252.08
CAS #
42079-78-7
Related CAS #
42079-78-7
Appearance
Yellow solid powder
LogP
3.5
tPSA
39.440
SMILES
COC1=CC=CC2=C1C(=O)C=C(O2)C3=CC=CC=C3
InChi Key
XRQSPUXANRGDAV-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H12O3/c1-18-13-8-5-9-14-16(13)12(17)10-15(19-14)11-6-3-2-4-7-11/h2-10H,1H3
Chemical Name
5-methoxy-2-phenylchromen-4-one
Synonyms
5-Methoxyflavone
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~125 mg/mL (198.2~495.5 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (8.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (8.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.9642 mL 19.8208 mL 39.6416 mL
5 mM 0.7928 mL 3.9642 mL 7.9283 mL
10 mM 0.3964 mL 1.9821 mL 3.9642 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
Contact Us Back to top