444939
MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem
The MEK1/2 Inhibitor, also referenced under CAS 305350-87-2, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem, SL327, Z-& E-α-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)benzeneacetonitrile
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About This Item
Empirical Formula (Hill Notation):
C16H12F3N3S
CAS Number:
Molecular Weight:
335.35
MDL number:
UNSPSC Code:
12352200
Quality Level
Assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
ethanol: 10 mg/mL
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK1/2 (IC50 = 180 nM and 220 nM, respectively). Shown to inhibit AP-1 activity (IC50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities at higher concentrations (IC50 >10 µM). Reported to offer neuroprotection against ischemic brain injury in mice by selectively blocking ERK1/2 activation. Also suppresses IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Uncompetitive with respect to ATP.
A cell-permeable, vinylogous cyanamide that acts as a selective inhibitor of MEK1 (IC50 = 180 nM) and MEK2 (IC50 = 220 nM). Also shown to inhibit AP-1 activity (IC50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities only at higher concentrations (IC50 >10 µM). Reported to exhibit neuroprotective effects against ischemic brain injury in mice by selectively blocking ERK1/2 activation (i.e. noncompetitive with respect to ATP). Also reported to suppress IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Supplied as a mixture of Z- and E-isomers.
Supplied as a mixture of Z- and E-isomers.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MEK 1, MEK 2
MEK 1, MEK 2
Product does not compete with ATP.
Reversible: no
Target IC50: 180 nM and 220 nM against MEK1 and MEK2, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Hetman, M., et al. 2002. J. Biol. Chem.277, 49577.
Ohno, M., et al. 2001. Nat. Neurosci.4, 1238.
Wang, H., et al. 2001. Biochem. Biophys. Res. Commun.286, 869.
Scherle, P.A., et al. 2000. J. Biol. Chem.275, 37086.
Valjent, E., et al. 2000. J. Neurosci.20, 8701.
Watabe, A.M., et al. 2000. J. Neurosci.20, 5924.
Atkins, C.M., et al. 1998. Nat. Neurosci.1, 602.
Ohno, M., et al. 2001. Nat. Neurosci.4, 1238.
Wang, H., et al. 2001. Biochem. Biophys. Res. Commun.286, 869.
Scherle, P.A., et al. 2000. J. Biol. Chem.275, 37086.
Valjent, E., et al. 2000. J. Neurosci.20, 8701.
Watabe, A.M., et al. 2000. J. Neurosci.20, 5924.
Atkins, C.M., et al. 1998. Nat. Neurosci.1, 602.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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