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QNZ (EVP4593)

现货
Catalog No.
A4217
强效NF-κB抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 700.00
现货
5mg
¥ 650.00
现货
25mg
¥ 2,600.00
现货

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Background

EVP4593 is an inhibitor of NF-κB pathway with IC50 value of 11nM [1].

EVP4593 is a quinazoline derivative. It is screened out from a luciferase reporter gene-based assay using human Jurkat T cells. EVP4593 is found as an inhibitor of PMA/PHA-induced NF-κB pathway. It shows significant inhibition of both NF-κB transcriptional activation and TNF-α production (IC50 value of 7nM). Additionally, EVP4593 also has anti-inflammatory efficacy. It inhibits edema formation in a rat carrageenin-induced paw edema model [1].

Since NF-κB pathway may play a direct role in Huntington’s disease (HD) pathogenesis, EVP4593 is found to have beneficial effects in Drosophila HD transgenic model. It significantly slows the progressive decline in the climbing speed without toxic effects [2].

References:
[1] Tobe M, Isobe Y, Tomizawa H, Nagasaki T, Takahashi H, Fukazawa T, Hayashi H. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. Bioorg Med Chem. 2003 Feb 6;11(3):383-91.
[2] Wu J, Shih HP, Vigont V, Hrdlicka L, Diggins L, Singh C, Mahoney M, Chesworth R, Shapiro G, Zimina O, Chen X, Wu Q, Glushankova L, Ahlijanian M, Koenig G, Mozhayeva GN, Kaznacheyeva E, Bezprozvanny. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment. Chem Biol. 2011 Jun 24;18(6):777-93.

文献引用

1. Yen TH, Hsieh CL, et al. "Amentoflavone Induces Apoptosis and Inhibits NF-ĸB-modulated Anti-apoptotic Signaling in Glioblastoma Cells." In Vivo. 2018 Mar-Apr;32(2):279-285. PMID:29475910
2.YU-CHANG LIU, RENG-HONG WU, et al. "Regorafenib diminishes the expression and secretion of angiogenesis and metastasis associated proteins and inhibits cell invasion via NF-κB inactivation in SK-Hep1 cells."Received February 19, 2016; Accepted January 12, 2017

Chemical Properties

StorageStore at -20°C
M.Wt356.42
Cas No.545380-34-5
FormulaC22H20N4O
Solubility≥15.05 mg/mL in DMSO, ≥10.06 mg/mL in EtOH with ultrasonic, <2.4 mg/mL in H2O
Chemical Name4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

YAC128中度多刺神经元原代培养

溶解方法

该化合物在DMSO中的溶解度大于15.05 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

300 nM

应用

在YAC128 MSN神经元中,HD(Huntington’s disease)的主要病理学区域,EVP4593(300 nM)强烈衰减储存的Ca2+流入(SOC)。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1] Wu J, Shih H P, Vigont V, et al. Neuronal store-operated calcium entry pathway as a novel therapeutic target for Huntington's disease treatment[J]. Chemistry & biology, 2011, 18(6): 777-793.

生物活性

描述 QNZ是一种NF-κB抑制剂,在人类Jurkat细胞中的IC50值为11 nM。
靶点 NF-κB          
IC50 11 nM (in human Jurkat cell line)          

质量控制

化学结构

QNZ (EVP4593)

相关生物数据

QNZ (EVP4593)

相关生物数据

QNZ (EVP4593)