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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: SL327, Z-& E-α-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)benzeneacetonitrile

Primary Target: MEK 1, MEK 2
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
305350-87-2C₁₆H₁₂F₃N₃S
Description
OverviewA 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.
Supplied as a mixture of Z- and E-isomers.
Catalogue Number444939
Brand Family Calbiochem®
SynonymsSL327, Z-& E-α-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)benzeneacetonitrile
References
ReferencesHetman, 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.
Product Information
CAS number305350-87-2
ATP CompetitiveN
FormOff-white solid
Hill FormulaC₁₆H₁₂F₃N₃S
Chemical formulaC₁₆H₁₂F₃N₃S
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetMEK 1, MEK 2
Primary Target IC<sub>50</sub>180 nM and 220 nM against MEK1 and MEK2, respectively
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
444939 0

Documentation

MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem Certificates of Analysis

TitleLot Number
444939

References

Reference overview
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.

Posters

Title
Human Kinome & InhibitorSelect™ Libraries
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision04-January-2010 RFH
SynonymsSL327, Z-& E-α-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)benzeneacetonitrile
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number305350-87-2
Chemical formulaC₁₆H₁₂F₃N₃S
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (200 mg/ml) or Ethanol (10 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Toxicity Standard Handling
ReferencesHetman, 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.