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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.