Home NF-κB NF-κB inhibitor - TNF-alpha inhibitor QNZ (EVP4593) For research use only.

QNZ (EVP4593)

QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.

QNZ (EVP4593) Chemical Structure

QNZ (EVP4593) Chemical Structure

CAS No. 545380-34-5

Purity & Quality Control

QNZ (EVP4593) Related Products

Signaling Pathway

NF-κB Signaling Pathways

NF-κB Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat Kinase assay ~10 μM causes NF-κB Inhibition with EC50 of 9 nM 21700213
Jurkat Function assay 3 μM causes SOC Inhibition 21700213
neurons Function assay 300 nM inhibit store-operated Ca2+ entry 21700213
SK-N-SH Function assay 300 nM inhibits TRPC1-Supported SOC Ca2+ currents 21700213
neurons Function assay 300 nM protect YAC128 MSN from glutamate toxicity 21700213
GABA MS-like neurons Function assay 100 nM rescues abnormal SOC-mediated calcium entry 27080129
GABA MS-like neurons Function assay 1000 nM normalizes the number of lysosomes/autophagosomes 27080129
GABA MS-like neurons Function assay 100 nM rescues aging neurons from cell death 27080129
HepG2 Function assay HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50 = 0.012 μM. 22586124
HepG2 Function assay 0.1 to 10 uM 1 hr Inhibition of TNFalpha-induced NFkappaB (unknown origin)-dependent transcriptional activity expressed in human HepG2 cells at 0.1 to 10 uM incubated for 1 hr prior to TNFalpha induction measured after 6 hrs by dual-luciferase reporter gene assay 23219854
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Biological Activity

Description QNZ (EVP4593) shows potent inhibitory activity toward both NF-κB activation and TNF-α production with IC50 of 11 nM and 7 nM in Jurkat T cells, respectively.
Targets
TNF-α [1]
(Jurkat T cells)		 NF-κB [1]
(Jurkat T cells)
7 nM 11 nM
In vitro
In vitro

EVP4593 inhibits TNF-a production from murine splenocytes stimulated with LPS with IC50 of 7 nM. [1]

EVP4593 (300 nM) entails a significant decrease of amplitude of store-operated currents (approximately by 60%), induced by application of 1 μM thapsigargin in Htt138Q cells, thus prevents abnormal store-operated calcium entry. EVP4593 is able to inhibit the activity of channels containing TRPC1 as one of the subunits, but has no effect on homooligomer channels composed exclusively of TRPC1. [2]

QNZ (40 nM) completely abolishes the enhancement of neurite number and length evoked by laminin treatment of the schwann cells. QNZ reduces the neurite length by 61.36% of the schwann cells. QNZ significantly inhibits laminin-induced neurite outgrowth. QNZ also greatly diminishes the neurite elongation after 72 hours culture implying that both initial sprouting and longer term growth and extension seen in response to schwann cells seeded on laminin is mediated by NF-κB. [3]

QNZ (10 nM) abolishes LPS-induced up-regulation of CSE expression in rat neutrophil. [4]

QNZ (100 nM) blocks the induction effects of GRO/KC on K currents in IB4-negative neurons. [5]
Kinase Assay NF-κB assay
Human Jurkat T cells are cultured at 37℃ in a 5% CO2 atmosphere in RPMI1640 containing 10% FCS. The cells are plated in 6-well plates (2×106/well) and transiently transfected using the SuperFect Transfection Reagent with 1 μg of pNFκB-Luc. After transfection, the cells are cultured at 37℃ overnight. They are then collected, resuspended in fresh medium, and plated in 96-well plates (2×105/well). EVP4593 is dissolved in DMSO and added at the appropriate concentrations to the 96-well plates containing the cells, and the plates are then incubated at 37℃ for 1 hour. For induction of transcription, 10 ng/mL of PMA and 100 μg/mL of PHA are added to each well, and the cells are incubated for an additional 6 hours at 37℃. The culture media are removed, and cell lysis buffer containing luciferase substrate is added to each well. The each portion is transferred to a black 96-well plate, and then luminescence is immediately measured with a Packard Topcount. The 50% inhibitory concentration (IC50) values are calculated by a nonlinear regression method.
Cell Research Cell lines Jurkat cells
Concentrations IC50 of 11 nM (NF-κB) and 7 nM (TNF-α)
Incubation Time 1 h
Method

Test compounds were dissolved in DMSO and added at the appropriate concentrations to the 96-well plates containing the cells, and the plates were then incubated at 37 C for 1 h
Experimental Result Images Methods Biomarkers Images PMID
Western blot NF-κB p65 / OPN / Tissue factor / Thrombin VEGF / TNF-α / IL-1β / IL-6 / MMP-2 / MMP-9 / NF-κB p65(Ser536) 29061995
Growth inhibition assay Cell viability 28693192
In Vivo
In vivo

EVP4593 (1 mg/kg, i.p.) dose-dependently inhibits carrageenin-induced paw edema in rats. [1]
Animal Research Animal Models male SD rats with carrageenin induced paw edema
Dosages 1 mg/kg
Administration intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 356.42 Formula

C22H20N4O
CAS No. 545380-34-5 SDF Download QNZ (EVP4593) SDF
Smiles C1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 7 mg/mL ( (19.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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