2,5-Dihydroxycinnamic Acid phenethyl ester (Synonyms:5-LOX-IN-2)
目录号 : KCM12062 CAS No. : 179691-97-5 纯度 : ≥98%
2,5-Dihydroxycinnamic acid phenethyl ester is an inhibitor of 5-lipoxygenase (5-LO) with an IC value of 0.33 µM for inhibition of 5-LO product synthesis in polymorphonuclear leukocytes (PMNLs) stimulated with the sarcoendoplasmic reticulum calcium ATPase (SERCA) inhibitor thapsigargin . It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (IC = 16.41 µM) in a cell-free assay. 2,5-Dihydroxycinnamic acid phenethyl ester selectively decreases viability of RCC4 and 786-O cells lacking the Von Hippel-Lindau (VHL) tumor suppressor gene (ICs = 8 and 34.8 µM, respectively) over cells homozygously expressing VHL (ICs = 99.6 and >100 µM, respectively). However, it also decreases viability of RCC10 VHL and RCC10 VHL cells (ICs = 5.04 and 0.96 µM, respectively). It increases the levels of pro-caspase-3a, LC3B-I, and LC3B-II in RCC4 VHL cells in a concentration-dependent manner.
规格 价格 是否有货 数量
10 mM * 1 mL in DMSO
In-stock
1mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock

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生物活性

2,5-Dihydroxycinnamic Acid phenethyl ester , an inhibitor of 5-lipoxygenase (5-LOX) with an IC50 of 0.33 μM, inhibits 5-LOX in a dose-dependent manner . 2,5-Dihydroxycinnamic Acid phenethyl ester, reduces the cell viability of renal cancer cells and induces apoptosis, can be used for cancer research.

IC50&Target

5-LOX

0.33 μM (IC50)

体外研究

2,5-dihydroxycinnamic Acid phenyl ester (0-100 μM; 4 days) can reduce the viability of renal cancer cells and is more selective towards RCC4 and 786.0 cells lacking the Von Hippel Lindau (VHL) tumor suppressor gene.
2,5-dihydroxycinnamic Acid phenyl ester (0-10 μM; 24 hours) can increase the expression of LC3B and p62, block autophagy flux in RCC4 cells, and induce apoptosis mediated cell death by activating the caspase-3 pathway.

 

Cell Viability Assay

Cell Line: RCC4, RCC10, 786.0 cells
Concentration: 0-100 μM
Incubation Time: 4 days
Result:
Reduced the cell viability of renal cancer cells and was more selective toward RCC4 and 786.0 cells which are deficient for the Von Hippel-Lindau (VHL) tumor suppressor gene.

Western Blot Analysis

Cell Line: RCC4, RCC10, 786.0 cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Increased in LC3B and p62 expression, blocked of the autophagic flux in RCC4 cells.
Stimulated in a dose ependent manner the cleavage of pro-caspase-3 only in the RCC4 cells which lack the VHL tumor suppressor.
分子式
C17H16O4
分子量
284.31
CAS号
179691-97-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro:

DMSO : 100 mg/mL (351.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5173 mL 17.5864 mL 35.1729 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 mL
10 mM 0.3517 mL 1.7586 mL 3.5173 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:10% DMSO  40% PEG300  5% Tween-80  45% saline

    Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.79 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
+
+
+

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积:

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。