U0126

U0126 속성

U0126 C화학적 특성, 용도, 생산

개요

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).

용도

U0126 is a MEK inhibitor.

정의

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.

일반 설명

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.

생물학적 활성

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™ .

U0126 준비 용품 및 원자재

원자재

준비 용품

U0126 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	47465	58
Zhengzhou Alfa Chemical Co.,Ltd	+8618530059196	sale04@alfachem.cn	China	12393	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Career Henan Chemica Co	+86-0371-86658258 15093356674;	laboratory@coreychem.com	China	30255	58
Shanghai UCHEM Inc.	+862156762820 +86-13564624040	sales@myuchem.com	China	6711	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Henan Aochuang Chemical Co.,Ltd.	+86-0371-63689365 +8618638391208	sales@aochuangchem.com	China	9425	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11681	58

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