U0126-EtOH

製品コード：S1102 純度：99.98%

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

CAS No. 1173097-76-1

サイズ	価格(税別)	在庫状況
25mg	JPY 22000	国内在庫あり
100mg	JPY 70500	国内在庫あり
1g	JPY 190500	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（762）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

U0126-EtOHと併用されることが多い化合物

SP600125

U0126-EtOH and SP600125 reverse several genes upregulation in RAW264.7 and Ana-1 cells caused by Echinococcus multilocularis soluble antigen.

Chong S, et al. Bioengineered. 2022 Apr;13(4):8747-8758.

Adezmapimod (SB203580)

U0126-EtOH and Adezmapimod ameliorate indoxyl sulfate-induced inhibitory effects and reductions in Kv4.2, Kv4.3, and KChIP2 proteins and genes.

Yang J, et al. JCI Insight. 2022 Feb 8; 7(3): e145475.

Purmorphamine

U0126-EtOH in the presence of Purmorphamine inhibits sonic hedgehog-induced levels of p-ERK1/2 in RA-FLSs.

Liu F, et al. Front Immunol. 2018 Dec 5;9:2847.

U0126-EtOH関連製品

関連ターゲット	MEK1 MEK1/2 MEK2 MEK5	もっと見る
関連製品	Mirdametinib (PD0325901) PD98059 PD184352 (CI-1040) BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 BIX 02188 GDC-0623 SL-327 Myricetin BI-847325 PD318088 APS-2-79 HCl	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

MEKシグナル伝達経路

MEK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
rat PC12 cells	Function assay	10 μM	1 h	Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with JNK inhibitor SP600125 for 1 hr before compound addition by Western blot analysis	21345685
mouse RAS-3T3 cells	Function assay	10-40 μM		Inhibition of MEK-mediated ERK1/2 phosphorylation in mouse RAS-3T3 cells at 10 to 40 uM by ELISA.	24507826
HCT116 cells	Function assay			Ability of compound to inhibit anchorage independent colony formation (soft agar growth assay) in HCT116 cells, IC50=19.4 μM.	15225706
COS-7 cells	Function assay			Inhibitory concentration against AP-1 transcription in COS-7 cells， IC50=1 μM.	15006386
HeLa cells	Function assay			Inhibition of EGF-stimulated Elk1-luciferase reporter assay in HeLa cells, IC50=0.29 μM.	15225706
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

特性

A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

Targets

MEK2 ^[1] (Cell-free assay)	MEK1 ^[1] (Cell-free assay)
0.06 μM	0.07 μM

In Vitro
In vitro	U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. ^[1] U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels. ^[2] A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK. ^[3]
Kinase Assay	In Vitro Kinase Assays
Kinase Assay	The amount of immunoprecipitated wild type MEK used in these assays is adjusted to give a similar amount of activity units as obtained with 10 nM recombinant MEK. Reaction velocities are measured using a 96-well nitrocellulose filter apparatus as described below. Unless otherwise noted, reactions are carried out at an enzyme concentration of 10 nM, in 20 mM Hepes, 10 mM MgCl₂, 5 mM β-mercaptoethanol, 0.1 mg/mL BSA, pH 7.4, at room temperature. Reactions are initiated by the addition of [γ-³³P]ATP into the premixed MEK/ERK/inhibitor reaction mixture, and an aliquot of 100 μL is taken every 6 minutes and transferred to the 96-well nitrocellulose membrane plate which has 50 mM EDTA to stop the reaction. The membrane plate is drawn and washed 4 times with buffer under vacuum. Wells are then filled with 30 μL of Microscint-20 scintillation fluid, and the radioactivity of ³³P-phosphorylated ERK is counted with a Top Count scintillation counter. Velocities are obtained from the slopes of radioactivity versus time plots. Concentrations of ERK and ATP are 400 nM and 40 μM, respectively, unless otherwise indicated. For all of the in vitro enzyme assays, the percent inhibition is calculated 100 (1 −Vi/Vo) where Vi and Vo are the initial reaction velocities in the presence and absence of inhibitor, respectively. The data are then plotted as percent inhibition as a function of inhibitor concentration and fit, by nonlinear least squares regression, to the standard equation for a Langmuir isotherm to determine the IC50. As reported, enzyme concentrations are based upon molecular weights and mass of protein used in the final assay volume and not on active site titration. Thus, the actual enzyme active site concentration may differ from that reported.
細胞実験	細胞株	A.E7 or Th17 cells
	濃度	0 to 10 μM
	反応時間	48 hours
	実験の流れ	A.E7 or Th17 cells are incubated with C-treated B10.BR or BALB/c splenocytes plus varying concentrations of pigeon cytochrome c or PR8 Ag, or with 5 U/mL human rIL-2. In addition, some assays contains U0126 or an inactive analogue, U0124, to determine direct effects of MEK inhibition on T cell proliferation. Two days after culture initiation, each well is pulsed with 1 µCi of [³H]TdR and harvested the following day. The incorporation of [³H]TdR into DNA is quantitated on a Packard Matrix 96 direct beta counter without the use of liquid scintillation mixtures.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-MEK / MEK / p-ERK / ERK E-cadherin / Vimentin / Twist-2		27487136
	Immunofluorescence	pERK / pPPARγ E-cadherin / Vimentin CD40		27145370

In Vivo
In Vivo	U0126-EtOH, as the inhibitor of intracellular Raf/MEK/ERK signaling pathway, demonstrates antiviral activity by suppressing propagation of the 2009 pandemic IV H1N1 variant and highly pathogenic avian influenza viruses (HPAIV) in vivo in the mouse lung by inhibiting. ^[4] U0126-EtOH shows the potential neuroprotective effect and improving spatial learning in Morris water maze (MWM) by activating peroxisome proliferator-activated receptor gamma coactivator-1a, nuclear respiratory factor 1, and mitochondrial transcription factor A in Aβ-injected rats. ^[5]
動物実験	動物モデル	Female C57Bl/6 mice infected by Mouse-adapted highly pathogenic avian influenza A/FPV/Bratislava/79 (H7N7; FPV) virus and swine origin human influenza A virus (SOIV) A/Regensburg/D6/2009 (H1N1v; RB1).
	投与量	≤10 mM
	投与経路	Administered via aerosol.

参考
[1] Duncia JV, et al. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844. [2] DeSilva DR, et al. J Immunol. 1998, 160(9), 4175-4181. [3] Freeman MR, et al. Cancer Biol Ther. 2011, 12(11), 966-977. [4] Droebner K, et al. Antiviral Res. 2011, 92(2), 195-203. [5] Ashabi G, et al. Behav Brain Res. 2012. [6] Favata MF, et al. J Biol Chem. 1998, 273(29), 18623-18632. + 展開

参考

+ 展開

化学情報

分子量	426.56	化学式	C₁₈H₁₆N₆S₂.C₂H₆O
CAS No.	1173097-76-1	SDF	Download U0126-EtOH SDFをダウンロードする
Smiles	CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 85 mg/mL ( (199.26 mM)；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

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よくある質問（FAQ）

質問1:
I want to know whether the compound is light-sensitive?

回答
S1102 U0126-EtOH is not stable. It should be stored as powder at -20°C, and prepared the solution just before use.

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):