For research use only.
Molecular Weight(MW): 244.24
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
Selleck's Piceatannol has been cited by 18 publications
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Change of protein and mRNA with or without the pretreatment of Syk inhibitors. After pretreated with PRT062607 and Piceatannol for 30 min before A. fumigatus hyphae stimulation, activation of Syk was inhibited by 1 μM PRT062607 (p < 0.05), 2 μM PRT062607 (p < 0.01), 5 μM Piceatannol (p < 0.05), 10 μM Piceatannol (p < 0.01) a compared with untreated cells. mRNA expression of IL-1β, IL-6, IL-8 and CXCL1 induced by A. fumigatus hyphae were significantly suppressed b. mRNA expression of IL-1β, IL-6, IL-8, CXCL1 downregulated significantly by 1 μM PRT062607, 2 μM PRT062607, 5 μM Piceatannol, 10 μM Piceatannol. **means p < 0.01, *p < 0.05.
BMC Ophthalmol, 2014, 15:56.. Piceatannol purchased from Selleck.
Influence of piceatannol and resveratrol on hydrogen peroxide production by human subcutaneous fat tissue. H202 release was monitored on a 30-min period without any added agent, except the chromogenic mixture (basal), or with NADPH oxidase inhibitor (apocynin 10 μM, shaded column), each stilbene at 1 mM, or MAO and SSAO inhibitors (pargyline plus semicarbazide at 1 mM: parg + semi, dotted column). Each column is the mean ± SEM of 16 homogenates from obese patients. Different from basal hydrogen peroxide production at: **P < 0.01.
Chem Biol Interact, 2016, 258:115-25. . Piceatannol purchased from Selleck.
Effect of acupuncture through Baihui (DU20) to Qubin (GB7) on brain histopathology of rats after intracerebral hemorrhage (hematoxylin and eosin staining, original magnification, 200×). (A) Sham group; (B) ICH group; (C) piceatannol group; (D) acupuncture group. Rats in the sham group had no blood injection into the brain, and showed no inflammatory infiltration (arrows) from the semi-dark area and normal microscopic features. Pathological features (arrows) in the ICH group were intracranial blood injection, tissue edema, partial nerve cell necrosis, glial cell swelling, intracellular vacuoles, and inflammatory cell infiltration. Pathological features (arrows) were less severe in rats receiving acupuncture or piceatannol treatment after blood injection. ICH: Intracerebral hemorrhage.
Neural Regen Res, 2018, 13(8):1425-1432. Piceatannol purchased from Selleck.
HCECs were preincubated for 30 min with syk inhibitor Piceatannol, followed by treatment with hyphae for 15 min. The activation of syk or PLCγ was assayed by Western Blot. Results shown are mean ± SD of three independent experiments. *p < 0.05, **p < 0.001.
BMC Ophthalmol, 2018, 18(1):170. Piceatannol purchased from Selleck.
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Choose Selective Syk Inhibitors
|Description||Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.|
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.  Piceatannol inhibits NF-κB activation induced by TNF, H2O2, PMA, LPS, okadaic acid, and ceramide. Piceatannol suppresses the expression of TNF-induced NF-κB-dependent reporter gene and of matrix metalloprotease-9, cyclooxygenase-2, and cyclin D1 independent of Syk kinase, by blocking TNF-induced IκBα phosphorylation, p65 phosphorylation, p65 nuclear translocation, and IκBα kinase activation.  Piceatannol directly binds with PI3K in an ATP-competitive manner, and suppresses PI3K activity with anti-atherosclerotic effects more effectively than resveratrol.  Piceatannol inhibits androgen-dependent (AD) and androgen-independent (AI) CaP cell proliferation, which is accompanied by reduced expression of mTOR and its key effectors AKT and eIF4EBP-1. 
|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. |
In Vitro Protein-tyrosine Kinase Assays: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.
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-  Wang BH, et al. Planta Med, 1998, 64(3), 195-199.
-  Su L, et al. J Biol Chem, 2000, 275(17), 12661-12666.
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-  Fernandez LA, et al. Transplantation, 2002, 74(11), 1609-1617.
-  Kim YH, et al. Int Immunopharmacol, 2008, 8(12), 1695-1702.
-  Choi KH, et al. Cardiovasc Res, 2010, 85(4), 836-844.
-  Minakawa M, et al. Biochem Biophys Res Commun, 2012, 422(3), 469-475.
-  Hsieh TC, et al. ISRN Urol, 2012, 272697.
|In vitro||DMSO||48 mg/mL (196.52 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40% PEG300+5% Tween+50%ddH2O
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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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.
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