product name
U0126, U0126, CAS 109511-58-2, is 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.
质量水平
检测方案
≥98% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
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°C
InChI
1S/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 key
DVEXZJFMOKTQEZ-JYFOCSDGSA-N
一般描述
MEK1（IC50=72 nM）和MEK2（IC50=58 nM）的有效和特异性抑制剂。这种抑制对ATP和ERK都是非竞争性的。对其他激酶如Abl、Cdk2、Cdk4、ERK、JNK、MEKK、MKK-3、MKK-4/SEK、MKK-6、PKC和Raf几乎没有影响。显示可阻断多沙唑嗪诱导的成骨细胞分化。也可作为免疫抑制剂，有效阻断IL-2合成和T细胞增殖，而不影响T细胞活化或耐受的长期结果。对于ATP没有竞争性。也可提供InSolution格式（目录号662009）。
MEK1（IC50=72 nM）和MEK2（IC50=58 nM）的有效和特异性抑制剂。这种抑制对MEK底物、ATP和ERK是非竞争性的。对其他激酶如Abl、Cdk2、Cdk4、ERK、JNK、MEKK、MKK-3、MKK-4/SEK、MKK-6、PKC和Raf几乎没有影响。显示可阻断多沙唑嗪诱导的成骨细胞分化。U0126还可作为免疫抑制剂，有效阻断IL-2合成和T细胞增殖，而不影响T细胞活化或耐受的长期结果。对于ATP没有竞争性。也可提供InSolution格式（目录号662009。
生化/生理作用
主靶
MEK1和MEK2
MEK1和MEK2
产物不与ATP竞争。
可逆：否
细胞可渗透性：否
靶标IC50：针对MEK1和MEK2分别为72和58nM。
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
溶液中不稳定；仅在使用前进行复溶。
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.
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
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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