Daphnetin

Catalog No.S2554 Batch:S255408

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Technical Data

Formula

C9H6O4
Molecular Weight 178.14 CAS No. 486-35-1
Solubility (25°C)* In vitro DMSO 36 mg/mL (202.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Kinase Assay:[1]
  • 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 Assay:[2]
  • 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.
Animal Study:[2]
  • Animal Models

    Immature CD1 (Im) female mice

  • Dosages

    35 mg/kg, 70 mg/kg, and 140 mg/kg

  • Administration

    Subcutaneously

Customer Product Validation

Data from [Data independently produced by , , Inflammation Research, 2017, 66(7):579-589]

Selleck's Daphnetin has been cited by 4 publications

Daphnetin ameliorates acute lung injury in mice with severe acute pancreatitis by inhibiting the JAK2-STAT3 pathway [ Sci Rep, 2021, 11(1):11491] PubMed: 34075160
Patient-derived organoids and orthotopic xenografts of primary and recurrent gliomas represent relevant patient avatars for precision oncology [ Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7] PubMed: 33009951
Daphnetin prevents methicillin-resistant Staphylococcus aureus infection by inducing autophagic response. [ Int Immunopharmacol, 2019, 72:195-203] PubMed: 30991161
Daphnetin reduces endotoxin lethality in mice and decreases LPS-induced inflammation in Raw264.7 cells via suppressing JAK/STATs activation and ROS production [Shen L, et al. Inflamm Res, 2017, 66(7):579-589] PubMed: 28409189

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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