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Butein

产品编号 T6427 CAS 487-52-5

别名: 2’,3,4,4’-tetrahydroxy Chalcone, 紫铆因

Butein (2’,3,4,4’-tetrahydroxy Chalcone) 是一种 cAMP 特异性PDE 抑制剂，也是蛋白酪氨酸激酶抑制剂，还是一种SIRT1激活剂。它通过 AKT 和 ERK/p38 MAPK 通路，靶向 FoxO3a 使 HeLa 细胞对 Cisplatin 敏感。

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Butein, CAS 487-52-5

规格	价格/CNY	货期
1 mg	￥ 296	现货
2 mg	￥ 429	现货
5 mg	￥ 698	现货
10 mg	￥ 963	现货
25 mg	￥ 1,960	现货
50 mg	￥ 3,680	待询
100 mg	￥ 5,290	待询
1 mL * 10 mM (in DMSO)	￥ 683	现货

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植物来源	天然产物 > 桑科 > 构树属

产品描述	Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.
靶点活性	p60c-src:65 μM, EGF:65 μM
体外活性	Butein inhibits the epidermal growth factor (EGF)-stimulated auto-phosphotyrosine level of EGF receptor in HepG2 cells, and also inhibits tyrosine-specific protein kinase activities of EGF receptor and p60c-src with IC50 of 65 μM in vitro. The inhibition is competitive to ATP and non-competitive to the phosphate acceptor, poly (Glu, Ala, Tyr) 6:3:1 for EGF receptor tyrosine kinase. In contrast, Butein non-significantly inhibits the activities of serine- and threonine-specific protein kinases such as PKC or PKA. [1] Butein inhibits Nuclear Factor(NF)-κB and NF-κB-regulated gene expression through direct inhibition of IκBα Kinase β on Cysteine 179 Residue. [2] Butein (10 μM) inhibits over 90% iNOS and COX-2 expression, as well as nitrite and TNF-α production in LPS-stimulated RAW 264.7 cells. Butein (10 μM) inhibits LPS-induced DNA binding activity of NF-κB, which is mediated through inhibition of the degradation of inhibitory factor-κB and phosphorylation of Erk1/2 MAP kinase, as well as increases binding of the osteopontin a vb3 integrin receptor. [3] Butein (20 μM) treatment induces morphologic changes of bladder cancer cells BLS(M) from elongated morphology to rounded epithelial-like cells, accompanied by downregulation of vimentin, and gaining of E-cadherin compared to untreated control cells, indicating the reversal of mesenchymal-like phenotype. Butein (20 μM) suppresses motility and invasion capacity of BLS(M) cells, and reverts EMT-like phenotype induced by TNF-α, through the ERK1/2 and NF-κB signaling pathways. [4]
体内活性	Butein at 2 mg/kg induces significant inhibition of hepatocellular tumor growth compared with the corn oil-treated controls. At necropsy on day 22 after initial treatment, there is more than 2-fold decrease in tumor growth in the Butein-treated group (mean relativetumor burden, 3.90) compared with the control group (8.46), associated with reduced constitutive p-STAT3 (9% vs 81% of vehicle group), Bcl-2 levels (26% vs 96% of vehicle group), and increased caspase-3 level (98% vs 21% of vehicle group) in HCC tumor tissues. [5] Butein shows antifibrogenic activity. Butein (25 mg/kg/day) reduces serum AST and ALT activation to 35% and 69%, respectively, of control CCl4-induced rat levels. Butein (25 mg/kg/day) reduces liver hydroxyproline contents and TBAR4 concentration to 54% and 54%, respectively. α1(I) collagen and TIMP-1 expression in Butein-treated rats is 28% and 20.3% compared with the values for the respective CCl4-treated control. [7]
细胞实验	The cells (5× 103/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Butein in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader. (Only for Reference)

别名	2’,3,4,4’-tetrahydroxy Chalcone, 紫铆因
分子量	272.25
分子式	C15H12O5
CAS No.	487-52-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 51 mg/mL (187.3 mM)

Ethanol: 51 mg/mL (187.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	3.6731 mL	18.3655 mL	36.7309 mL	91.8274 mL
	5 mM	0.7346 mL	3.6731 mL	7.3462 mL	18.3655 mL
	10 mM	0.3673 mL	1.8365 mL	3.6731 mL	9.1827 mL
	20 mM	0.1837 mL	0.9183 mL	1.8365 mL	4.5914 mL
	50 mM	0.0735 mL	0.3673 mL	0.7346 mL	1.8365 mL
	100 mM	0.0367 mL	0.1837 mL	0.3673 mL	0.9183 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Yang EB, et al. Biochem Biophys Res Commun, 1998, 17, 245(2), 435-438. 2. Pandey MK, et al. J Biol Chem, 2007, 282(24), 17340-17350. 3. Lee SH, et al. Biochem Biophys Res Commun, 2004 , 323(1), 125-132. 4. Zhang L, et al. FEBS Lett, 2008, 582(13), 1821-1828. 5. Rajendran P, et al. Clin Cancer Res, 2011, 17(6), 1425-1439. 6. Zhang L, et al. Butein sensitizes HeLa cells to cisplatin through the AKT and ERK/p38 MAPK pathways by targeting FoxO3a.Int J Mol Med. 2015 Oct;36(4):957-66.

文献引用

1. Zhao L, Zhang W, Luan F, et al.Butein suppresses PD-L1 expression via downregulating STAT1 in non-small cell lung cancer.Biomedicine & Pharmacotherapy.2023, 157: 114030.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Butein 487-52-5 Angiogenesis Apoptosis Autophagy JAK/STAT signaling Metabolism Others Tyrosine Kinase/Adaptors EGFR PDE PDE4 Epidermal growth factor receptor Inhibitor MAPK 2’,3,4,4’-tetrahydroxy Chalcone ErbB-1 FoxO3a inhibit cell SIRT1 Phosphodiesterase (PDE) ERK PKB AKT HeLa HER1 p38 紫铆因 HepG2 inhibitor

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Butein

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

Keywords