444937
MEK Inhibitor I
The MEK Inhibitor I, also referenced under CAS 297744-42-4, controls the biological activity of MEK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
MEK Inhibitor I
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关于此项目
经验公式（希尔记法）:
C21H18N4OS
化学文摘社编号:
分子量:
374.46
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
产品名称
MEK Inhibitor I, The MEK Inhibitor I, also referenced under CAS 297744-42-4, controls the biological activity of MEK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
assay
≥95% (sum of two isomers, HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 10 mg/mL
methanol: 50 mg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MEK
MEK
Product does not compete with ATP.
Reversible: no
Target IC50: 12 nM against MEK
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable pyridine-containing vinylogous cyanamide compound that acts as a potent and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 >1 µM). The inhibition is noncompetitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. noncompetitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
A cell-permeable, potent, and selective inhibitor of MEK (IC50 = 12 nM) with little activity towards MKK3 and MKK4 (IC50 >1 µM). The inhibition is non-competitive with respect to ERK and the compound displays significant affinity only towards ATP-bound MEK (i.e. non-competitive with respect to ATP). Exhibits superior potency, solubility, and stability compared to U0126 (Cat. No. 662005) in aqueous solutions. Shown to protect against phorbol ester-mediated ear edema in mice (ED50 of 5 mg/kg, ip.).
Other Notes
Wityak, J., et al. 2004. Bioorg. Med. Chem. Lett.14, 1483.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Gretchen M Argast et al.
Cells, tissues, organs, 193(1-2), 114-132 (2010-11-03)
Epithelial to mesenchymal transition (EMT) plays a dual role in tumor progression. It enhances metastasis of tumor cells by increasing invasive capacity and promoting survival, and it decreases tumor cell sensitivity to epithelial cell-targeting agents such as epithelial growth factor
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