QNZ (EVP4593)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EVP4593是NF-κB途径的抑制剂，其IC50值是11 nM[1]。
EVP4593是一种喹唑啉衍生物。EVP4593是在人类Jurkat T细胞中基于荧光酶报告基因的检测而筛选出来的。EVP4593是一种PMA/PHA诱导的NF-κB途径的抑制剂。EVP4593对NF-κB的转录激活和TNF-α的生成（IC50值为7 nM）都有显著的抑制作用。此外，EVP4593也具有抗炎作用，在卡拉胶诱导的大鼠足肿胀模型中可阻止水肿形成[1]。
由于NF-κB途径可能在亨廷顿氏病（HD）的发病机理中扮演直接的作用，EVP4593在果蝇HD转基因模型中被发现存在正向效应。EVP4593显著地阻碍了爬坡速度的逐渐下降，而不产生毒性效应[2]。
参考文献：
[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.
- 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
| Storage | Store at -20°C |
| M.Wt | 356.42 |
| Cas No. | 545380-34-5 |
| Formula | C22H20N4O |
| Solubility | insoluble in H2O; ≥10.06 mg/mL in EtOH with ultrasonic; ≥15.05 mg/mL in DMSO |
| Chemical Name | 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
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细胞系 |
YAC128中度多刺神经元原代培养 |
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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。 |
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反应条件 |
300 nM |
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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）。 |
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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。 |
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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. |
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| 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) | |||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
