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Piceatannol
別名：Astringenin
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
CAS No. 10083-24-6
文献中Selleckの製品使用例（34）
製品安全説明書
現在のバッチを見る：
純度：
99.49%
99.49
Piceatannol関連製品
シグナル伝達経路
Syk阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| mouse 3T3L1 cells | Function assay | 10 to 50 μM | 48 h | Reduction in triglyceride level in mouse 3T3L1 cells at 10 to 50 uM after 48 hrs | 22765896 |
| human A2780 cells | Proliferation assay | 2 days | Antiproliferative activity against human A2780 cells after 2 days by Alamar Blue assay, IC50=41 μM | 24239390 | |
| human lung mast cells | Function assay | Inhibition of SYK in human lung mast cells assessed as reduction in anti-IgE-stimulated histamine release, EC50=25 μM | 22257213 | ||
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生物活性
| 製品説明 | Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn. | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| 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] | |||
|---|---|---|---|---|
| Kinase Assay | 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. | ||||
| 細胞実験 | 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. |
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| In Vivo | ||
| 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] | |
|---|---|---|
| 動物実験 | 動物モデル | Female BALB/c mice with dextran sulfate sodium (DSS)-induced colitis |
| 投与量 | ~10 mg/kg/day | |
| 投与経路 | Orally | |
化学情報
| 分子量 | 244.24 | 化学式 | C14H12O4 |
| CAS No. | 10083-24-6 | SDF | Download Piceatannol SDFをダウンロードする |
| Smiles | C1=CC(=C(C=C1C=CC2=CC(=CC(=C2)O)O)O)O | ||
| 保管 | |||
|
In vitro |
DMSO : 48 mg/mL ( (196.52 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 48 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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