Daphnetin

Catalog No.S2554

Daphnetin Chemical Structure

Molecular Weight(MW): 178.14

Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.

Size Price Stock Quantity  
In DMSO USD 70 In stock
USD 50 In stock
USD 120 In stock
USD 210 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.
Targets
EGFR [1] PKA [1] PKC [1]
7.67 μM 9.33 μM 25.01 μM
In vitro

Daphnetin strongly inhibits not only EGF receptor-catalyzed tyrosine phosphorylation of exogenous substrate but also PKA and PKC activities. [1] Daphnetin inhibits MCF-7 estrogen-responsive human carcinoma cell line at 24-hour exposure with IC50 of 73 μM. Daphnetin reduces the level of cyclin D1 even at 50 μM. [2] Daphnetin protects the cortical neurons against dexamethasone-induced reduction of cell viability in a dose-dependent manner. [3] Daphnetin inhibits the activities of endogenous or recombinant TaPRK in a specific and dose-dependent manner. [4] daphnetin causes a 50% inhibition (IC50) of 3H-hypoxanthine incorporation by Plasmodium falciparum at concentrations between 25 μM and 40 μM. [5] Daphnetin inhibits the mitogenic signalling of ERK1/ERK2. [6]

In vivo Daphnetin at 140 mg/kg significantly decreases uterine weights by 39.5%. [2] Two and 8 mg/kg administration of Daphnetin could improve the performance of stress mice in Morris water maze tests and forced swimming tests. [3] Daphnetin significantly prolongs survival of P. yoelli-infected mice. [5]

Protocol

Kinase Assay:[1]
+ Expand

Assay of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) activities.:

PKC and PKA activities are detected. Briefly, 5 mL of PKC or PKA is mixed with 5 mL of lipid preparation containing 100 mM phorbol 12-myristate 13-acetate, 2.8 mg/mL phosphatidyl serine, and Triton X-100 mixed micelles for PKC assay or 5 mL of 40 mM cAMP in 50 mM Tris-HCl, pH 7.5, for PKA assay, and 5 mL of daphnetin. The reaction is started by adding 10 mL of PKC substrate solution containing 250 mM acetylated myelin basic protein, 100 mM ATP, 5 mM CaCl2, 10 mM MgCl2, 20 mM Tris-HCl, pH 7.5, or 10 mL of PKA substrate solution containing 200 mM Kemptide, 400 mM ATP, 40 mM MgCl2, 1 mg/mL BSA, 50 mM Tris-HCl, pH 7.5, and 20-25 mCi/mL[g-32P] ATP. After incubation at 25 °C for 5 minutes, 20 mL of each mixture is spotted on a piece of phosphocellulose disc which is immediately put into 1% H3PO4. After free [g-32P] ATP on the discs is removed, the peptide-incorporated 32P on the discs is counted in a scintillation counte
Cell Research:[2]
+ Expand
  • Cell lines: MCF-7 cells
  • Concentrations: 12.5 μM, 25 μM, 50 μM, 100 μM, 200 μM
  • Incubation Time: 24 hours, 48 hours, and 72 hours
  • Method: The cytostatic effect of Daphnetin tested on the MCF-7 tumor cells is estimated using the microculture MTT assay. The assay is based on the reduction of soluble tetrazolium salt by mitochondria of viable cells. The reduced product, an insoluble purple-colored formazan, is dissolved in dimethyl sulfoxide and measured spectrophotometrically (570 nm). The amount of formazan formed is proportional to the number of viable cells. Cells (3 × 103) are seeded in each of the 96 microplate wells in a 200 μL medium containing the corresponding concentration of daphnetin. Daphnetin is tested at five concentrations (12.5 μM, 25 μM, 50 μM, 100 μM, 200 μM). After 24-hour, 48-hour, and 72-hour exposure, the percentage of proliferative inhibition of treated cells is estimated against the solvent-treated control cells (PI% = [(T/C) − 1] × 100). PI = proliferation inhibition; T = treated, C = control. IC50 is calculated from the least square concentration-response regressions.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Immature CD1 (Im) female mice
  • Formulation: Corn oil
  • Dosages: 35 mg/kg, 70 mg/kg, and 140 mg/kg
  • Administration: Subcutaneously
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 35 mg/mL (196.47 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 178.14
Formula

C9H6O4

CAS No. 486-35-1
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

EGFR Signaling Pathway Map

Related EGFR Products

Tags: buy Daphnetin | Daphnetin supplier | purchase Daphnetin | Daphnetin cost | Daphnetin manufacturer | order Daphnetin | Daphnetin distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID