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444939 MEK Inhibitor VII - CAS 305350-87-2 - Calbiochem

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      Overview

      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
      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
      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
      Global Trade Item Number
      Catalogue Number GTIN
      444939 0