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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.
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
white
溶解度
DMSO: 200 mg/mL
運輸包裝
ambient
儲存溫度
−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 密鑰
DVEXZJFMOKTQEZ-JYFOCSDGSA-N
一般說明
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。
包裝
用惰性气体包装
警告
毒性：标准处理（A）
重構
溶液中不稳定；仅在使用前进行复溶。
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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