Piceatannol

製品コードS3026 バッチS302605

印刷

化学情報

Chemical Structure Synonyms Astringenin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H12O4
分子量 244.24 CAS No. 10083-24-6
Solubility (25°C)* 体外 DMSO 48 mg/mL (196.52 mM)
Ethanol 48 mg/mL (196.52 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween 50%ddH2O
4.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 LNCaP, DU145, and PC-3
濃度 Dissolved in DMSO, final concentrations ~50 μM
反応時間 72 hours and 1 week
実験の流れ

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.
動物実験 動物モデル Female BALB/c mice with dextran sulfate sodium (DSS)-induced colitis
投薬量 ~10 mg/kg/day
投与方法 Orally

カスタマーフィードバック

, , BMC Ophthalmol, 2014, 15:56.

Data from [Data independently produced by , , Chem Biol Interact, 2016, 258:115-25. ]

Data from [Data independently produced by , , Neural Regen Res, 2018, 13(8):1425-1432]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Polyaniline-Based Glyco-Condensation on Au Nanoparticles Enhances Immunotherapy in Lung Cancer [ ACS Appl Mater Interfaces, 2022, 14(21):24144-24159] PubMed: 35579575
Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer [ Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9] PubMed: 36271983
Global post-translational modification profiling of HIV-1-infected cells reveals mechanisms of host cellular pathway remodeling [ Cell Rep, 2022, 38(13):110567] PubMed: 35354044
Main Determinants Affecting the Antiproliferative Activity of Stilbenes and Their Gut Microbiota Metabolites in Colon Cancer Cells: A Structure-Activity Relationship Study [ Int J Mol Sci, 2022, 23(23)15102] PubMed: 36499424
Orientia tsutsugamushi Infection Stimulates Syk-Dependent Responses and Innate Cytosolic Defenses in Macrophages [ Pathogens, 2022, 12(1)53] PubMed: 36678402
Orientia tsutsugamushi Infection Stimulates Syk-Dependent Responses and Innate Cytosolic Defenses in Macrophages [ Pathogens, 2022, 12(1)53] PubMed: 36678402
CCL4-mediated targeting of spleen tyrosine kinase (Syk) inhibitor using nanoparticles alleviates inflammatory bowel disease [ Clin Transl Med, 2021, 11(2):e339] PubMed: 33634985
TREM1 Regulates Neuroinflammatory Injury by Modulate Proinflammatory Subtype Transition of Microglia and Formation of Neutrophil Extracellular Traps via Interaction With SYK in Experimental Subarachnoid Hemorrhage [ Front Immunol, 2021, 12:766178] PubMed: 34721438
Inhibition of Dectin-1 Ameliorates Neuroinflammation by Regulating Microglia/Macrophage Phenotype After Intracerebral Hemorrhage in Mice [ Transl Stroke Res, 2021, 10.1007/s12975-021-00889-2] PubMed: 33539006
Polyphenols and Cannabidiol Modulate Transcriptional Regulation of Th1/Th2 Inflammatory Genes Related to Canine Atopic Dermatitis [ Front Vet Sci, 2021, 8:606197] PubMed: 33763461

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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