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产品说明

一般描述

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.
A potent and specific inhibitor of MEK1 (IC50 = 72 nM) and MEK2 (IC50 = 58 nM). The inhibition is noncompetitive with respect to both 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. 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).

包装

1, 5 mg in Glass bottle
10, 20 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
MEK1 and MEK2
Product does not compete with ATP.
Target IC50: 72 nM, 58 nm, against MEK1, and MEK2, respectively
Reversible: no
Cell permeable: no

警告

Toxicity: Standard Handling (A)

重悬

Unstable in solution; reconstitute just prior to use.

其他说明

Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun.416, 232.
DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett.8, 2839.
Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C18H16N6S2 · 0.5C2H6O
分子量403.52
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 200 mg/mL
运输ambient
储存温度−20℃
InChI1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+
InChI keyDVEXZJFMOKTQEZ-JYFOCSDGSA-N

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 2
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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