QNZ (EVP4593)

製品コード：S4902 純度：99.94%

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.

CAS No. 545380-34-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（132）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

QNZ (EVP4593)関連製品

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関連化合物ライブラリー	FDA-approved Drug Library Immunology/Inflammation Compound Library Small Molecule Immuno-Oncology Compound Library NF-κB Signaling Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

NF-κBシグナル伝達経路

NF-κB阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
neurons	Function assay	300 nM		protect YAC128 MSN from glutamate toxicity	21700213
SK-N-SH	Function assay	300 nM		inhibits TRPC1-Supported SOC Ca2+ currents	21700213
neurons	Function assay	300 nM		inhibit store-operated Ca2+ entry	21700213
Jurkat	Function assay	3 μM		causes SOC Inhibition	21700213
Jurkat	Kinase assay	~10 μM		causes NF-κB Inhibition with EC50 of 9 nM	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
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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.

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
Kinase 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.
細胞実験	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	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
実験結果図	Methods	Biomarkers	結果図	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]
動物実験	動物モデル	male SD rats with carrageenin induced paw edema
	投与量	1 mg/kg
	投与経路	intraperitoneal injection

参考
[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. [3] Armstrong SJ, et al. Neurosci Lett, 2008, 439(1), 42-46. [4] Li L, et al. J Cell Mol Med, 2009, 13(8B), 2684-2692. [5] Yang RH, et al. Mol Pain, 2009, 28(5), 26. + 展開

参考

+ 展開

化学情報

分子量	356.42	化学式	C₂₂H₂₀N₄O
CAS No.	545380-34-5	SDF	Download QNZ (EVP4593) SDFをダウンロードする
Smiles	C1=CC=C(C=C1)OC2=CC=C(C=C2)CCNC3=NC=NC4=C3C=C(C=C4)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 7 mg/mL ( (19.63 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):