U0126

한글명:U0126

카스 번호109511-58-2

상품명:U0126

CBNumberCB4758734

분자식C18H16N6S2

포뮬러 무게380.49

MOL 파일109511-58-2.mol

화학적 성질

녹는점	approximate 154℃(dec.)
끓는 점	565.1±50.0 °C(Predicted)
밀도	1.44
RTECS 번호	EJ9710000
저장 조건	Desiccate at +4°C
용해도	DMSO에 용해됩니다(최대 200mg/ml).
물리적 상태	흰색 고체
산도 계수 (pKa)	2.11±0.10(Predicted)
색상	하얀색
수용성	DMSO에 용해됩니다. 에탄올과 물에 잘 녹지 않음
안정성	제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO의 솔루션은 -20°에서 최대 3개월 동안 보관할 수 있습니다.

위험 및 안전 성명

HS 번호

2930909899

그림문자(GHS)

U0126 화학적 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™ .

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