product name Piceatannol
Description: Piceatannol, a natural stilbene, is a potent and selective Syk inhibitor and ~10-fold selectivity versus Lyn. It also has anti-inflammatory, immunomodulatory and antiproliferative activities. It inhibits p56lck and syk protein tyrosine kinases and inhibits TNF-induced NF-κB activation and gene expression. Synthesis results from conversion of resveratrol by cytochrome P450 1B1.
References: J Biol Chem. 1994 Nov 25;269(47):29697-703.; Int Immunopharmacol. 2008 Dec 10;8(12):1695-702.
244.24
Formula
C14H12O4
CAS No.
10083-24-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (196.5 mM)
Water: <1 mg/mL
Ethanol: <48 mg/mL (196.5 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Piceatannol displays ~10-fold selectivity for Syk over Lyn. Piceatannol treatment in RBL-2H3 cells strongly inhibits the antigen-stimulated phosphorylation of Syk and of most other cellular proteins but not the receptor β or γ subunit, in a dose-dependent manner. Piceatannol is also a potent inhibitor of histamine release in mast cells. Selective inhibition of Syk by Piceatannol blocks receptor-mediated down-stream cellular responses in mast cells including prevention of 1,4,5-IP3 synthesis, secretion and membrane ruffling and spreading. Piceatannol also potently inhibits PKA, PKC, MLCK, and CDPK with IC50 of 3 μM, 8 μM, 12 μM, and 19 μM, respectively. Piceatannol selectively prevents the IFNα-induced tyrosine phosphorylation of STAT3 and -5 but not STAT1 and -2, paralleled by the loss of Jak1 and IFNAR1 tyrosine phosphorylation but not Tyk2 and IFNAR2. Piceatannol potently induces apoptotic cell death in BJAB Burkitt-like lymphoma cells with ED50 of 25 μM, through the activation of caspase-3 and mitochondrial permeability transition independent of the CD95/Fas signaling pathway. Kinase Assay: Recombinant Syk is expressed in baculovirus-infected St9 cells. Assays of recombinant Syk activity are carried out using angiotensin I peptide as substrate. The enzyme activities of recombinant Syk are measured by phosphorylation of angiotensin I peptide in the presence of various concentrations of Piceatannol. Cell Assay: Cells (LNCaP, DU145, and PC-3) are exposed to increasing concentrations of Piceatannol. For the determination of cell proliferation, cells are assayed at 72 hours by trypan blue exclusion using a hemocytometer. After 1 week, colonies are stained with 1.25% crystal violet and quantified by measuring the absorbance at 595 nm. |
|---|---|
| In Vivo | Oral administration of Piceatannol induces a remarkable amelioration of the disruption of the colonic architecture, a significant reduction in colonic myeloperoxidase (MPO) activity, and a decrease in production of inflammatory mediators such as nitric oxide (NO), prostaglandin (PG) E2, and pro-inflammatory cytokines in BALB/c mice with dextran sulfate sodium (DSS)-induced colitis. Piceatannol treatment inhibits the rises in blood glucose levels at early stages and improves the impaired glucose tolerance at late stages in type 2 diabetic model db/db mice. |
| Animal model | Female BALB/c mice with dextran sulfate sodium (DSS)-induced colitis |
| Formulation & Dosage | Dissolved in DMSO, and diluted in corn oil;10 mg/kg; oral administration |
| References | J Biol Chem. 1994 Nov 25;269(47):29697-703.; Int Immunopharmacol. 2008 Dec 10;8(12):1695-702. |
