您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Q-VD-OPH
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Q-VD-OPH
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Q-VD-OPH图片
CAS NO:1135695-98-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Quinoline-Val-Asp-Difluorophenoxymethylketone
产品介绍
Q-VD-OPh 是一种具有强效抗凋亡特性的泛半胱天冬酶抑制剂。它可抑制HIV感染,能透过血脑屏障。

产品描述

Q-VD-OPha is a pan-caspase inhibitor with potent antiapoptotic properties.

体外活性

Q-VD-OPh (5-100 μM) potently inhibits Actinomycin D-induced DNA laddering and subsequent apoptosis with minimal toxicity in WEHI 231 cells. Q-VD-OPh prevents caspase mediated cleavage of PARP and activation of the major initiator and effector caspases. [2] Q-VD-OPh protects cardiac myocytes from virus-induced apoptosis in vitro. [4]

体内活性

Q-VD-OPh inhibits caspase-1 activity, IL-18 protein expression, and neutrophil infiltration during ischemic ARF in mice. [3] In vivo, caspase inhibition by Q-VD-OPh provides protection from virus-induced myocardial injury, with a significant reduction in caspase-3 activity. [4] In TgCRND8 mice, Q-VD-OPh inhibits caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. [5]

激酶实验

Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200?000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1].

细胞实验

Caspase inhibitors are added at the indicated concentrations 30 minutes prior to the addition of apoptotic stimuli. Viability and cell number are determined by trypan blue exclusion from three random fields of greater than 200 cells/field. All experiments are performed a minimum of three times.(Only for Reference)

Cas No.

1135695-98-5

分子式

C26H25F2N3O6

分子量

513.498

别名

Quinoline-Val-Asp-Difluorophenoxymethylketone

储存和溶解度

Ethanol:100 mg/mL (194.75 mM)
DMSO:25 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years