Myricetin

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Chemical Structure| 529-44-2 同义名 : Cannabiscetin; LDN-0014058; HSDB 7682; NSC 407290
CAS号 : 529-44-2
货号 : A268149
分子式 : C15H10O8
纯度 : 98%
分子量 : 318.24
MDL号 : MFCD00006827
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(94.27 mM)，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

无水乙醇: 25 mg/mL(78.56 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
生物活性
靶点

  • MEK1
描述 PI3Kγ signalling through Akt and mTor inhibits NFκB activation while stimulating C/EBPβ (CCAAT/enhancer binding protein) activation, thereby inducing a transcriptional program that promotes immune suppression during inflammation and tumour growth[3]. Myricetin has a Kd of 0.17 μM for PI3Kγ[4]. As one of the major flavonols in red wine, myricetin is also a novel inhibitor of MEK1 (mitogen-activated protein kinase) activity and transformation of JB6 P+ mouse epidermal cells. Myricetin (10 mM) inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA) or epidermal growth factor (EGF)-induced cell transformation by 76 or 72%, respectively. It strongly inhibited MEK1 kinase activity and suppressed TPA- or EGF-induced phosphorylation of extracellular signal-regulated kinase (ERK) or p90 ribosomal S6 kinase, downstream targets of MEK. Moreover, myricetin inhibited H-Ras-induced cell transformation[5]. Myricetin inhibits viability of SKOV3 ovarian cancer cells in a dose-dependent manner. It induces DNA DSBs and ER stress, which leads to apoptosis in SKOV3 cells[6]. Exposure to 150 μM myricetin causes 14%, 26%, 5% and 49% inhibition of rabbit platelet aggregation, induced by ADP, arachidonic acid, collagen and PAF (platelet-activating factor), respectively[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=4.1 μM 22212721
HeLa cells Function assay Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM 19725578
HT-29 cells Function assay Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=2.12 μM 24900447
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.71mL

3.14mL

1.57mL

31.42mL

6.28mL

3.14mL
参考文献

[1]Phillips PA, Sangwan V, et al. Myricetin induces pancreatic cancer cell death via the induction of apoptosis and inhibition of the phosphatidylinositol 3-kinase (PI3K) signaling pathway. Cancer Lett. 2011 Sep 28;308(2):181-8.

[2]Knekt P, Kumpulainen J, et al. Flavonoid intake and risk of chronic diseases. Am J Clin Nutr. 2002 Sep;76(3):560-8.

[3]Kaneda MM, Messer KS, Ralainirina N, Li H, Leem CJ, Gorjestani S, Woo G, Nguyen AV, Figueiredo CC, Foubert P, Schmid MC, Pink M, Winkler DG, Rausch M, Palombella VJ, Kutok J, McGovern K, Frazer KA, Wu X, Karin M, Sasik R, Cohen EE, Varner JA. PI3Kγ is a molecular switch that controls immune suppression. Nature. 2016 Nov 17;539(7629):437-442. doi: 10.1038/nature19834. Epub 2016 Sep 19. Erratum in: Nature. 2017 Feb 2;542(7639):124. PMID: 27642729; PMCID: PMC5479689.

[4]Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, Wymann MP, Williams RL. Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. Mol Cell. 2000 Oct;6(4):909-19. doi: 10.1016/s1097-2765(05)00089-4. PMID: 11090628.

[5]Lee KW, Kang NJ, Rogozin EA, Kim HG, Cho YY, Bode AM, Lee HJ, Surh YJ, Bowden GT, Dong Z. Myricetin is a novel natural inhibitor of neoplastic cell transformation and MEK1. Carcinogenesis. 2007 Sep;28(9):1918-27. doi: 10.1093/carcin/bgm110. Epub 2007 Aug 11. PMID: 17693661.

[6]Xu Y, Xie Q, Wu S, Yi D, Yu Y, Liu S, Li S, Li Z. Myricetin induces apoptosis via endoplasmic reticulum stress and DNA double-strand breaks in human ovarian cancer cells. Mol Med Rep. 2016 Mar;13(3):2094-100. doi: 10.3892/mmr.2016.4763. Epub 2016 Jan 12. PMID: 26782830; PMCID: PMC4768956.

[7]Tzeng SH, Ko WC, Ko FN, Teng CM. Inhibition of platelet aggregation by some flavonoids. Thromb Res. 1991 Oct 1;64(1):91-100. doi: 10.1016/0049-3848(91)90208-e. PMID: 1776142.