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Daphnetin Europäischer Partner

ArtNr S2554-50
Hersteller Selleckchem
CAS-Nr. 486-35-1
Menge 50 mg
Quantity options 10 mg 1 g 10 g 10 mM/1 ml 25 mg 50 mg 5 g
Kategorie
Typ Inhibitors
Specific against other
Smiles C1=CC(=C(C2=C1C=CC(=O)O2)O)O
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias 486-35-1'
Similar products Daphnetin
Lieferbar
Manufacturer - Targets
EGFR
Storage Conditions
2 years -80 in solvent
Molecular Weight
178, 14
Administration
Subcutaneously
Animal Models
Immature CD1 (Im) female mice
Cell lines
MCF-7 cells
Concentrations
12.5 uM, 25 uM, 50 uM, 100 uM, 200 uM
Dosages
35 mg/kg, 70 mg/kg, and 140 mg/kg
Formulation
Corn oil
IC50
7.67 uM, 7.67 uM, 7.67 uM, 7.67 uM, 7.67 uM, 7.67 uM
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 uM. Daphnetin reduces the level of cyclin D1 even at 50 uM. [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 uM and 40 uM. [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]
Incubation Time
24 hours, 48 hours, and 72 hours
Kinase Assay
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 25C 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 counter.
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 uL medium containing the corresponding concentration of daphnetin. Daphnetin is tested at five concentrations (12.5 uM, 25 uM, 50 uM, 100 uM, 200 uM). 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.
Solubility (25C)
DMSO 36 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information
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.

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 50 mg
Lieferbar: In stock
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