UO-126 化学構造式

UO-126

化学名:UO-126

CAS番号.109511-58-2

英語名:U0126

CBNumberCB4758734

MFC18H16N6S2

MW380.49

MOL File109511-58-2.mol

别名

U-0126

2,3-ビス[[(2-アミノフェニル)チオ]アミノメチレン]スクシノニトリル

ビス({[(2-アミノフェニル)スルファニル]アミノ}メチリデン)ブタンジニトリル

UO-126物理性質

融点	approximate 154℃(dec.)
沸点	565.1±50.0 °C(Predicted)
比重(密度)	1.44
RTECS 番号	EJ9710000
貯蔵温度	Desiccate at +4°C
溶解性	DMSO に可溶 (最大 200 mg/ml)。
外見	白い固体
酸解離定数(Pka)	2.11±0.10(Predicted)
色	白い
水溶解度	DMSOに可溶。エタノールと水に溶けにくい
安定性：	-20°C の DMSO 溶液で最大 3 か月間保存できます。

安全性情報

HSコード

2930909899

危険有害性情報のコード(GHS)

UO-126 価格

製品番号	包装	価格	製品説明	購入
富士フイルム和光純薬株式会社(wako) W01TOC1144	5mg	￥80000		購入
富士フイルム和光純薬株式会社(wako) W01BVI1668-5	5mg	￥33800		購入
富士フイルム和光純薬株式会社(wako) W01W0121-0105	5mg	￥29200	95.0+% (HPLC)(mixture of isomers)	購入
富士フイルム和光純薬株式会社(wako) W01TOC1144	25mg	￥326000		購入
関東化学株式会社(KANTO) 49077-08	25mg	￥140000		購入

UO-126 化学特性,用途語,生産方法

外観
白色～うすい褐色, 結晶～粉末
溶解性
アセトニトリルに可溶。エタノールに溶ける。DMSOに溶ける：100mmol/L
用途
MAPキナーゼカスケード阻害剤。
使用上の注意
不活性ガス封入
説明
U-0126 is a MEK inhibitor with IC₅₀ values of 72 nM and 58 nM for MEK1 and MEK2, respectively. It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3, MKK-4, MKK-6, Cdk2, and Cdk4. However, U-0126 does phosphorylate and activate AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC₅₀ = 15 μM in HEK293 cells). It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).
使用
U0126 is a MEK inhibitor.
定義
ChEBI: A dinitrile that is succinonitrile in which the methylene hydrogens at positions 2 and 3 are substituted by (2-aminophenyl)sulfanyl]methylidene groups. A potent and selective non-competitive inhibitor of MAP kinase kinase.
一般的な説明
A potent and specific inhibitor of MEK1 (IC₅₀ = 72 nM) and MEK2 (IC₅₀ = 58 nM). The inhibition is noncompetitive with respect to MEK substrates, ATP and ERK. Has very little effect on other kinases, such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Shown to block doxazosin-induced osteoblastic differentiation. U0126 also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Noncompetitive with respect to ATP. Also available in InSolution format (Cat. No. 662009.
生物活性
Potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC 50 values of 0.07 and 0.06 μ M respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Centrally active following systemic administration in vivo . Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™ .

UO-126 生産企業

109511-58-2, UO-126 キーワード

Send Inquriy