For research use only.

Catalog No.S3026

27 publications

Piceatannol Chemical Structure

CAS No. 10083-24-6

Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.

Selleck's Piceatannol has been cited by 27 publications

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Biological Activity

Description Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
Syk [1]
(Cell-free assay)
Lyn [1]
(Cell-free assay)
cAK [2]
(Cell-free assay)
PKC [2]
(Cell-free assay)
MLCK [2]
(Cell-free assay)
3 μM 8 μM 12 μM
In vitro

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. [1] Piceatannol also potently inhibits PKA, PKC, MLCK, and CDPK with IC50 of 3 μM, 8 μM, 12 μM, and 19 μM, respectively. [2] 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. [3] 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. [4] 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. [5] Piceatannol directly binds with PI3K in an ATP-competitive manner, and suppresses PI3K activity with anti-atherosclerotic effects more effectively than resveratrol. [8] 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. [10]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human lung mast cells MW\GeY5kfGmxbjDhd5NigQ>? NYG0TIsxUW6qaXLpeIlwdiCxZjDTXWshcW5iaIXtZY4hdHWwZzDtZZN1KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDhcpRqNUmpRT3zeIlufWyjdHXkJIhqe3SjbXnu[UBz\WynYYPlMEBGSzVyPUK1JO69VQ>? M13q[VIzOjV5MkGz
human A2780 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 MYiyJIRigXN? NWTudHkxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjCyJIRigXNiYomgRYxidWG{IFLseYUh[XO|YYmsJGlEPTB;NEGg{txO MnLVNlQzOzl|OUC=
mouse 3T3L1 cells NX7yN3dxTnWwY4Tpc44h[XO|YYm= NWDp[|VrOTBidH:gOVAh|ryP MUO0PEBp MYTS[YR2[3Srb36gbY4hfHKrZ3z5Z4VzcWSnIHzleoVtKGmwIH3veZNmKDOWM1yxJINmdGy|IHH0JFExKHSxIEWwJJVOKGGodHXyJFQ5KGi{cx?= MnfSNlI4PjV6OU[=

... Click to View More Cell Line Experimental Data

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. [7] 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. [9]


Kinase Assay:


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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.
Cell Research:


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  • Cell lines: LNCaP, DU145, and PC-3
  • Concentrations: Dissolved in DMSO, final concentrations ~50 μM
  • Incubation Time: 72 hours and 1 week
  • Method:

    Cells 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: Female BALB/c mice with dextran sulfate sodium (DSS)-induced colitis
  • Dosages: ~10 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 48 mg/mL (196.52 mM)
Water Insoluble
Ethanol '48 mg/mL
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.
4 mg/mL

* 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 244.24


CAS No. 10083-24-6
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=C(C=C1C=CC2=CC(=CC(=C2)O)O)O)O

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID