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QNZ (EVP4593)

Potent NF-κB inhibitor CAS# 545380-34-5

QNZ (EVP4593)

Catalog No. BCC2249----Order now to get a substantial discount!

Product Name & Size Price Stock
QNZ (EVP4593):5mg $120.0 In stock
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Chemical structure

QNZ (EVP4593)

3D structure

Chemical Properties of QNZ (EVP4593)

Cas No. 545380-34-5 SDF Download SDF
PubChem ID 509554 Appearance Powder
Formula C22H20N4O M.Wt 356.42
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EVP4593
Solubility DMSO : ≥ 37 mg/mL (103.81 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
SMILES C1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
Standard InChIKey IBAKVEUZKHOWNG-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H20N4O/c23-17-8-11-21-20(14-17)22(26-15-25-21)24-13-12-16-6-9-19(10-7-16)27-18-4-2-1-3-5-18/h1-11,14-15H,12-13,23H2,(H,24,25,26)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of QNZ (EVP4593)

DescriptionQNZ is an inhibitor of NF-κB with IC50 value of 11 nM in human Jurkat cells.
TargetsNF-κB    
IC5011 nM (in human Jurkat cell line)     

Protocol

Cell Assay [2]
iPSHD22 cells are cultured in K-4 medium in a 96-well black plates with clear flat bottom. Next, cells are treated with chemical compounds (e.g., QNZ 100 nM) for 24 h prior to analysis. Fluorescent assay MultiTox-Fluor Multiplex Cytotoxicity Assay is used to measure simultaneously the relative number of live (viability) and dead (cytotoxicity) cells in each well. Fluorescence is detected by DTX 880 Multimode Microplate Reader. To evaluate the level of cell death (LoCD), the following equation is employed: ([cytotoxicity in a well with cells]-[cytotoxicity in a well without cells])/([viability in a well with cells]-[viability in a well without cells])[2].

References:
[1]. Tobe M, et al. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation. [2]. Nekrasov ED, et al. Manifestation of Huntington's disease pathology in human induced pluripotent stem cell-derived neurons. Mol Neurodegener. 2016 Apr 14;11:27. [3]. Wu J, et al. Enhanced Store-Operated Calcium Entry Leads to Striatal Synaptic Loss in a Huntington's Disease Mouse Model. J Neurosci. 2016 Jan 6;36(1):125-41.

QNZ (EVP4593) Dilution Calculator

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QNZ (EVP4593) Molarity Calculator

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Preparing Stock Solutions of QNZ (EVP4593)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8057 mL 14.0284 mL 28.0568 mL 56.1136 mL 70.142 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL 11.2227 mL 14.0284 mL
10 mM 0.2806 mL 1.4028 mL 2.8057 mL 5.6114 mL 7.0142 mL
50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.1223 mL 1.4028 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.5611 mL 0.7014 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on QNZ (EVP4593)

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.

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References on QNZ (EVP4593)

Regorafenib induces extrinsic and intrinsic apoptosis through inhibition of ERK/NF-kappaB activation in hepatocellular carcinoma cells.[Pubmed:28000898]

Oncol Rep. 2017 Feb;37(2):1036-1044.

The aim of the present study was to investigate the role of NF-kappaB inactivation in regorafenib-induced apoptosis in human hepatocellular carcinoma SK-HEP-1 cells. SK-HEP-1 cells were treated with different concentrations of the NF-kappaB inhibitor 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine (QNZ) or regorafenib for different periods. The effects of QNZ and regorafenib on cell viability, expression of NF-kappaB-modulated anti-apoptotic proteins and apoptotic pathways were analyzed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, western blotting, DNA gel electrophoresis, flow cytometry and NF-kappaB reporter gene assay. Inhibitors of various kinases including AKT, c-Jun N-terminal kinase (JNK), P38 and extracellular signal-regulated kinase (ERK) were used to evaluate the mechanism of regorafenib-induced NF-kappaB inactivation. The results demonstrated that both QNZ and regorafenib significantly inhibited the expression of anti-apoptotic proteins and triggered extrinsic and intrinsic apoptosis. We also demonstrated that regorafenib inhibited NF-kappaB activation through ERK dephosphorylation. Taken all together, our findings indicate that regorafenib triggers extrinsic and intrinsic apoptosis through suppression of ERK/NF-kappaB activation in SK-HEP-1 cells.

The pentavalent antimonial therapy against experimental Leishmania amazonensis infection is more effective under the inhibition of the NF-kappaB pathway.[Pubmed:26218282]

Int Immunopharmacol. 2015 Sep;28(1):554-9.

During Leishmania infection, host immune response is important to prevent the growth/survival of intracellular amastigotes. In this study, we evaluated in vitro and in vivo whether or not during Leishmania amazonensis infection, pentavalent antimonial treatment/therapy could be more effective under TNF-alpha inhibition. Both L. amazonensis-infected macrophages (in vitro model) and mice (in vivo model) were treated with a nuclear factor-kappaB (NF-kappaB) inhibitor and with Glucantime(R), alone and in combined administrations. The in vitro amastigote counts, cytokines and nitrites' production were assessed after 48h incubation with the drugs. Paw lesion sizes and amastigote counts were also evaluated in vivo. Quantification of IL-1beta from the infected tissue was performed. In vitro results show that when infected macrophages were incubated with QNZ+Glucantime(R), a greater clearance was observed for the amastigotes' growth and this was related to greater nitrite production compared to the group that was only infected. In vivo results show that mice that received the combined treatment had their paw lesion sizes and amastigote nests inside the macrophages greatly diminished, correlating with increased IL-1beta levels.

Description

QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.

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