产品说明书

Piceatannol

Print
Chemical Structure| 10083-24-6 同义名 : Astringenin;trans-Piceatannol;NSC 622471;trans-3,3',4,5'-Tetrahydroxystilbene;trans-Picetannol
CAS号 : 10083-24-6
货号 : A162917
分子式 : C14H12O4
纯度 : 98%
分子量 : 244.243
MDL号 : MFCD00221715
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 100 mg/mL(409.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5%DMSO+40% PEG300+5% Tween+50%water 4 mg/mL

生物活性
靶点

  • Syk
描述 Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors[3]. Piceatannol, an anti-inflammatory, immunomodulatory, and anti-proliferative stilbene, is a selective Syk inhibitor, about 10-fold more sensitive than Lyn[4]. The treatment of human myeloid cells with piceatannol suppressed TNF-induced DNA binding activity of NF-κB. TNF-induced NF-κB activation was also suppressed in lymphocyte and epithelial cells. It also inhibited NF-κB activated by H2O2, PMA, LPS, okadaic acid, and ceramide[5]. In rat ventricular cells, piceatannol (3 - 30 µmol/L) prolonged the action potential durations (APDs) and decreased the maximal rate of upstroke (Vmax) without altering Ca2+ transients. Piceatannol (1 – 10 µmol/L) exerted antiarrhythmic activity in isolated rat hearts subjected to ischaemia‐reperfusion injury[6]. Oral piceatannol administration in BALB/c mice with dextran sulfate sodium (DSS)-induced colitis was associated with 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[7]. Piceatannol suppressed the rises in blood glucose levels at early stages and improved the impaired glucose tolerance at late stages in db/db mice[8].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
mouse 3T3L1 cells 10 to 50 μM Function assay 48 h Reduction in triglyceride level in mouse 3T3L1 cells at 10 to 50 uM after 48 hrs 22765896
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.94mL

8.19mL

4.09mL
参考文献

[1]Wang BH, Lu ZX, Polya GM. Inhibition of eukaryote serine/threonine-specific protein kinases by piceatannol. Planta Med. 1998 Apr;64(3):195-9

[2]Oliver JM, Burg DL, et al. Inhibition of mast cell Fc epsilon R1-mediated signaling and effector function by the Syk-selective inhibitor, piceatannol. J Biol Chem. 1994 Nov 25;269(47):29697-703.

[3]Liu D, Mamorska-Dyga A. Syk inhibitors in clinical development for hematological malignancies. J Hematol Oncol. 2017 Jul 28;10(1):145. doi: 10.1186/s13045-017-0512-1. PMID: 28754125; PMCID: PMC5534090.

[4]Oliver JM, Burg DL, Wilson BS, McLaughlin JL, Geahlen RL. Inhibition of mast cell Fc epsilon R1-mediated signaling and effector function by the Syk-selective inhibitor, piceatannol. J Biol Chem. 1994 Nov 25;269(47):29697-703. PMID: 7961959.

[5]Ashikawa K, Majumdar S, Banerjee S, Bharti AC, Shishodia S, Aggarwal BB. Piceatannol inhibits TNF-induced NF-kappaB activation and NF-kappaB-mediated gene expression through suppression of IkappaBalpha kinase and p65 phosphorylation. J Immunol. 2002 Dec 1;169(11):6490-7. doi: 10.4049/jimmunol.169.11.6490. PMID: 12444159.

[6]Chen WP, Hung LM, Hsueh CH, Lai LP, Su MJ. Piceatannol, a derivative of resveratrol, moderately slows I(Na) inactivation and exerts antiarrhythmic action in ischaemia-reperfused rat hearts. Br J Pharmacol. 2009 Jun;157(3):381-91. doi: 10.1111/j.1476-5381.2008.00106.x. Epub 2009 Apr 3. PMID: 19371352; PMCID: PMC2707985.

[7]Kim YH, Kwon HS, Kim DH, Cho HJ, Lee HS, Jun JG, Park JH, Kim JK. Piceatannol, a stilbene present in grapes, attenuates dextran sulfate sodium-induced colitis. Int Immunopharmacol. 2008 Dec 10;8(12):1695-702. doi: 10.1016/j.intimp.2008.08.003. Epub 2008 Sep 4. PMID: 18773974.

[8]Minakawa M, Miura Y, Yagasaki K. Piceatannol, a resveratrol derivative, promotes glucose uptake through glucose transporter 4 translocation to plasma membrane in L6 myocytes and suppresses blood glucose levels in type 2 diabetic model db/db mice. Biochem Biophys Res Commun. 2012 Jun 8;422(3):469-75. doi: 10.1016/j.bbrc.2012.05.017. Epub 2012 May 10. PMID: 22579688.