QNZ (EVP4593)

Catalog No.S4902 Batch:S490204

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Technical Data

Formula

C22H20N4O
Molecular Weight 356.42 CAS No. 545380-34-5
Solubility (25°C)* In vitro DMSO 71 mg/mL (199.2 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.55mg/ml Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Homogeneous suspension
0.5% hydroxyethyl cellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% hydroxyethyl cellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
In vivo

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

Protocol (from 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. 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 Assay:

[1]
  • 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
Animal Study:

[1]
  • Animal Models

    male SD rats with carrageenin induced paw edema

  • Dosages

    1 mg/kg

  • Administration

    intraperitoneal injection

Customer Product Validation

, , Cell Death Dis, 2018, 9(6):587

Data from [Data independently produced by , , Oncogene, 2018, 37(7):873-883]

Data from [Data independently produced by , , Cell Physiol Biochem, 2017, 41(1):91-100]

Data from [Data independently produced by , , Nephrol Dial Transplant, 2016: 1–9.]

Selleck's QNZ (EVP4593) has been cited by 149 publications

Tumor-derived apoptotic extracellular vesicle-mediated intercellular communication promotes metastasis and stemness of lung adenocarcinoma [ Bioact Mater, 2024, 36:238-255] PubMed: 38481566
BTLA contributes to acute-on-chronic liver failure infection and mortality through CD4+ T-cell exhaustion [ Nat Commun, 2024, 15(1):1835] PubMed: 38418488
PD-L1-expressing tumor-associated macrophages are immunostimulatory and associate with good clinical outcome in human breast cancer [ Cell Rep Med, 2024, 5(2):101420] PubMed: 38382468
Oncogenic KEAP1 mutations activate TRAF2-NFκB signaling to prevent apoptosis in lung cancer cells [ Redox Biol, 2024, 69:103031] PubMed: 38184997
TRPM2-mediated feed-forward loop promotes chondrocyte damage in osteoarthritis via calcium-cGAS-STING-NF-κB pathway [ J Adv Res, 2024, S2090-1232(24)00499-5] PubMed: 39505144
Whitening of brown adipose tissue inhibits osteogenic differentiation via secretion of S100A8/A9 [ iScience, 2024, 27(2):108857] PubMed: 38303710
Ferulic acid suppresses the inflammation and apoptosis in Kawasaki disease through activating the AMPK/mTOR/NF-κB pathway [ Front Pharmacol, 2024, 15:1420602] PubMed: 39268468
A Dendrimer Peptide (KK2DP7) Delivery System with Dual Functions of Lymph Node Targeting and Immune Adjuvants as a General Strategy for Cancer Immunotherapy [ Adv Sci (Weinh), 2023, 10(15):e2300116] PubMed: 36950751
Hepatic DDAH1 mitigates hepatic steatosis and insulin resistance in obese mice: Involvement of reduced S100A11 expression [ Acta Pharm Sin B, 2023, 13(8):3352-3364] PubMed: 37655336
A noncanonical response to replication stress protects genome stability through ROS production, in an adaptive manner [ Cell Death Differ, 2023, 10.1038/s41418-023-01141-0] PubMed: 36869180

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.