662005
U0126
≥98% (HPLC), solid, MEK inhibitor, Calbiochem®
别名:
U0126, 1,4-二氨基-2,3-二氰基-1,4-双(2-氨基苯巯基)丁二烯，d，MEK抑制剂VI
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关于此项目
经验公式（希尔记法）:
C18H16N6S2 · 0.5C2H6O
化学文摘社编号:
分子量:
403.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
产品名称
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.
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
S(c2c(cccc2)N)\C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)\N
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
General description
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
Biochem/physiol Actions
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。
Packaging
用惰性气体包装
Preparation Note
溶液中不稳定；仅在使用前进行复溶。
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
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存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable