QNZ (EVP4593)

Catalog No.S4902

QNZ (EVP4593) Chemical Structure

Molecular Weight(MW): 356.42

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.

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Cited by 29 Publications

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat MlrJT4lv[XOnIHHzd4F6 M2S4Np4yOCEQvF2= MXvjZZV{\XNiTl[t{tpDKEmwaHnibZRqd25id3n0bEBGSzVyIH;mJFkhdk1? NEXtO3gzOTdyMEKxNy=>
Jurkat MVzGeY5kfGmxbjDhd5NigQ>? Mn;vN{DPxE1? NFr4d4hk[XW|ZYOgV29EKEmwaHnibZRqd25? MlqxNlE4ODB{MUO=
neurons MlzySpVv[3Srb36gZZN{[Xl? M4m2fFMxOCCwTR?= MU\pcohq[mm2IIP0c5JmNW:yZYLheIVlKEOjMjug[Y51enl? NH60bnEzOTdyMEKxNy=>
SK-N-SH NYjXSnF2TnWwY4Tpc44h[XO|YYm= MXWzNFAhdk1? MVHpcohq[mm2czDUVnBEOS2VdYDwc5J1\WRiU1;DJGNiOitiY4XydoVvfHN? NUfs[Fd{OjF5MECyNVM>
neurons MVTGeY5kfGmxbjDhd5NigQ>? M2Lte|MxOCCwTR?= NYLXeHJ1eHKxdHXjeEB[SUNzMkigUXNPKG[{b32g[4x2fGGvYYTlJJRwgGmlaYT5 M2C4ZVIyPzByMkGz
GABA MS-like neurons NEPkTZFHfW6ldHnvckBie3OjeR?= Mn7qNVAxKG6P M2LCbJJme2O3ZYOgZYJvd3KvYXygV29ENW2nZHnheIVlKGOjbHPpeY0h\W62com= Mnn3NlcxQDBzMkm=
GABA MS-like neurons M{PZN2Z2dmO2aX;uJIF{e2G7 MmfzNVAxOCCwTR?= Mlr2co9zdWGuaYrld{B1cGViboXtZoVzKG:oIHz5d49{d22ncz;heZRweGijZ3;zc41mew>? MVuyO|A5ODF{OR?=
GABA MS-like neurons NX;qR3ZZTnWwY4Tpc44h[XO|YYm= MXqxNFAhdk1? M{Lre5Jme2O3ZYOgZYdqdmdibnX1do9veyCocn;tJINmdGxiZHXheIg> NF3uXWQzPzB6MEGyPS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
NF-κB p65 / OPN / Tissue factor / Thrombin ; 

PubMed: 29061995     


Hep3B-CCN3 cells treated with NFκB inhibitor EVP4593 or Aspirin exhibited a significant down regulation of OPN, TF, and thrombin, and the gels/blots in each group were cropped from different gels and different fields.

VEGF / TNF-α / IL-1β / IL-6 / MMP-2 / MMP-9 / NF-κB p65(Ser536) ; 

PubMed: 28693192     


Changes in protein expression levels including VEGF, TNF-α, IL-1β, IL-6, MMP-2, MMP-9, active form of NF-κB p65 [NF-κB p65 (Ser 536)] and total NF-κB p65 (NF-κB p65) were demonstrated with western blotting. aP<0.01 and bP<0.05 vs. control. VEGF, vascular endothelial growth factor; TNF-α, tumor necrosis factor α; IL, interleukin; MMP, matrix metalloproteinase; NF-κB p65, nuclear factor-κB tumor protein 65; DMSO, dimethyl sulfoxide; QNZ, 4-N-[2-(4-phenoxyphenyl) ethyl] quinazoline-4, 6-diamine.

29061995 28693192
Growth inhibition assay
Cell viability; 

PubMed: 28693192     


Change of cell viability was evaluated with MTT assay. **P<0.01 vs. control.

28693192
In vivo EVP4593 (1 mg/kg, i.p.) dose-dependently inhibits carrageenin-induced paw edema in rats. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: male SD rats with carrageenin induced paw edema
  • Formulation: 0.5% hydroxypropyl cellulose
  • Dosages: 1 mg/kg
  • Administration: intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (14.02 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.42
Formula

C22H20N4O

CAS No. 545380-34-5
Storage powder
in solvent
Synonyms N/A

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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.

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NF-κB Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID