Piceatannol

Catalog No.S3026

For research use only.

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

Piceatannol Chemical Structure

CAS No. 10083-24-6

Selleck's Piceatannol has been cited by 30 publications

Purity & Quality Control

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Biological Activity

Description Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
Targets
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)
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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 MX7GeY5kfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKFO\SzDpckBpfW2jbjDseY5oKG2jc4SgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGGwdHmtTYdGNXO2aX31cIF1\WRiaHnzeIFucW6nIILlcIVie2VuIFXDOVA:OjVizszN MV:yNlI2PzJzMx?=
human A2780 cells M1f1UHBzd2yrZnXyZZRqd25iYYPzZZk> MUKyJIRigXN? NF6xdVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIFnfGW{IEKg[IF6eyCkeTDBcIFu[XJiQnz1[UBie3OjeTygTWM2OD12MTFOwG0> NGmxR4YzPDJ|OUO5NC=>
mouse 3T3L1 cells MXnGeY5kfGmxbjDhd5NigQ>? M2nW[VExKHSxIEWwJO69VQ>? MXS0PEBp M{HYWnJm\HWldHnvckBqdiC2cnnncJlk\XKrZHWgcIV3\WxiaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOTBidH:gOVAhfU1iYX\0[ZIhPDhiaILz NHfp[2YzOjd4NUi5Oi=>
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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[10]

  • 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.

Animal Research:

[7]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 244.24
Formula

C14H12O4

CAS No. 10083-24-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1C=CC2=CC(=CC(=C2)O)O)O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

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Tech Support

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.

Handling Instructions

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