662005
U0126
≥98% (HPLC), solid, MEK inhibitor, Calbiochem®
別名:
U0126, 1,4-Diamino-2,3-dicyano-1,4- bis(2-aminophenylthio)butadiene, MEK Inhibitor VI, 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI
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この商品について
実験式（ヒル表記法）:
C18H16N6S2 · 0.5C2H6O
CAS番号:
分子量:
403.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
製品名
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.
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
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
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
Biochem/physiol Actions
Cell permeable: no
Primary Target
MEK1 and MEK2
MEK1 and MEK2
Product does not compete with ATP.
Reversible: no
Target IC50: 72 nM, 58 nm, against MEK1, and MEK2, respectively
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.
Packaging
Packaged under inert gas
Preparation Note
Unstable in solution; reconstitute just prior to use.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
General description
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).
保管分類
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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関連コンテンツ
An Introduction to Inhibitors and Their Biological Applications
グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 662005-1MGCN | 07790788052249 |
| 662005-10MGCN | 04055977261691 |
| 662005-5MGCN | 04055977261011 |
| 662005-20MGCN | 04055977261004 |
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