QNZ (EVP4593)

Catalog No.S4902

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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QNZ (EVP4593) Chemical Structure

QNZ (EVP4593) Chemical Structure
Molecular Weight: 356.42

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Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
JurkatNYLkUo1kU2mwYYPlJIF{e2G7NGP0SlV,OTBizszNM{HhToNifXOnczDOSk3PwkJiSX7obYJqfGmxbjD3bZRpKEWFNUCgc4YhQSCwTR?=NVrtPZVrOjF5MECyNVM>
JurkatNHLQNHlHfW6ldHnvckBie3OjeR?=NUm2TmdsOyEQvF2=Mlm0Z4F2e2W|IGPPR{BKdmirYnn0bY9vMnvDNlE4ODB{MUO=
neuronsM4\QcGZ2dmO2aX;uJIF{e2G7Mmm3N|AxKG6PNGDHS5BqdmirYnn0JJN1d3KnLX;w[ZJifGWmIFPhNksh\W62com=M{i0S|IyPzByMkGz
SK-N-SHMljJSpVv[3Srb36gZZN{[Xl?NYPnRmw6OzByIH7NNWnx[lZZcW6qaXLpeJMhXFKSQ{GtV5VxeG:{dHXkJHNQSyCFYUKrJIN2enKnboTzMV[yNVcxODJzMx?=
neuronsNIXPOY9HfW6ldHnvckBie3OjeR?=MXyzNFAhdk1?MlnCdJJwfGWldDDZRWMyOjhiTWPOJIZzd21iZ3z1eIFu[XSnIITvfIlkcXS7NX;mbplNOjF5MECyNVM>
GABA MS-like neuronsNITzSHJHfW6ldHnvckBie3OjeR?=NYHpcVhkOTByIH7NMYny[ZNkfWW|IHHico9zdWGuIGPPR{1u\WSrYYTl[EBk[WylaYXtJIVvfHK7NEfwOFAzPzB6MEGyPS=>
GABA MS-like neuronsNULZbFlYTnWwY4Tpc44h[XO|YYm=NGnxTpkyODByIH7NM3foZo5wem2jbHn6[ZMhfGinIH71cYJmeiCxZjDsfZNwe2:vZYOvZZV1d3CqYXfvd49u\XN?MXGyO|A5ODF{OR?=
GABA MS-like neuronsMmTXSpVv[3Srb36gZZN{[Xl?NUn5OFA3OTByIH7NMVny[ZNkfWW|IHHnbY5oKG6ndYLvcpMh\nKxbTDj[YxtKGSnYYToMlfENlcxQDBzMkm=

... Click to View More Cell Line Experimental Data

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

Protocol(Only for Reference)

Kinase Assay: [1]

NF-κB assay Human Jurkat T cells are cultured at 37℃ in a 5% CO2 atmosphere in RPMI1640 containing 10% FCS, 100 U/mL of penicillin, and 100 μg/mL of streptomycin. 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.

Animal Study: [1]

Animal Models male SD rats with carrageenin induced paw edema
Formulation 0.5% hydroxypropyl cellulose
Dosages 1 mg/kg
Administration intraperitoneal injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tobe M, et al. Bioorg Med Chem, 2003, 11(3), 383-391.

[2] VA Vigont, et al. Biochemistry (Mosc), 2012, 6(2), 206-214.

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Chemical Information

Download QNZ (EVP4593) SDF
Molecular Weight (MW) 356.42
Formula

C22H20N4O

CAS No. 545380-34-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 5 mg/mL warming (14.02 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% hydroxyethyl cellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 4,6-Quinazolinediamine, N4-[2-(4-phenoxyphenyl)ethyl]-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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