QNZ (EVP4593)

製品コードS4902 バッチS490204

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₂₀N₄O

分子量

356.42

CAS No.

545380-34-5

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

71 mg/mL (199.2 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% hydroxyethyl cellulose この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (28.06mM)	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.550mg/ml (9.96mM)	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.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
in vitro	QNZ (EVP4593) inhibits TNF-a production from murine splenocytes stimulated with LPS with IC50 of 7 nM. ^[1] This compound (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. It 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] At 40 nM, it 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. It significantly inhibits laminin-induced neurite outgrowth. This compound 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] It (10 nM) abolishes LPS-induced up-regulation of CSE expression in rat neutrophil. ^[4] At 100 nM, it blocks the induction effects of GRO/KC on K currents in IB4-negative neurons. ^[5]
in vivo	QNZ (EVP4593) dose-dependently inhibits carrageenin-induced paw edema in rats at 1 mg/kg (i.p.). ^[1]

製品説明

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.

in vitro

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

This compound (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. It 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]

At 40 nM, it 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. It significantly inhibits laminin-induced neurite outgrowth. This compound 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]

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

At 100 nM, it blocks the induction effects of GRO/KC on K currents in IB4-negative neurons. ^[5]

in vivo

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

プロトコル(参考用のみ)

キナーゼアッセイ	NF-κB assay
キナーゼアッセイ	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). QNZ (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. 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.
細胞アッセイ	細胞株	Jurkat cells
	濃度	IC50 of 11 nM (NF-κB) and 7 nM (TNF-α)
	反応時間	1 h
	実験の流れ	QNZ (EVP4593) was 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
動物実験	動物モデル	male SD rats with carrageenin induced paw edema
	投薬量	1 mg/kg
	投与方法	intraperitoneal injection

参考

https://pubmed.ncbi.nlm.nih.gov/12517433/
http://link.springer.com/article/10.1134/S199074781201014X
https://pubmed.ncbi.nlm.nih.gov/18502047/

https://pubmed.ncbi.nlm.nih.gov/19120693/
https://pubmed.ncbi.nlm.nih.gov/19476648/

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カスタマーフィードバック

: , , 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]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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