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328007 ERK Inhibitor II, FR180204 - CAS 865362-74-9 - Calbiochem

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      Overview

      Key Spec Table

      CAS #Empirical Formula
      865362-74-9C₁₈H₁₃N₇
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC50 = 510 nM and 330 nM; Ki = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC50 = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC50 = 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available as a 10 mM solution in DMSO (Cat. No. 328010).

      Catalogue Number328007
      Brand Family Calbiochem®
      Synonyms5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
      References
      ReferencesOhori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.
      Product Information
      CAS number865362-74-9
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₈H₁₃N₇
      Chemical formulaC₁₈H₁₃N₇
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetERK1 and ERK2
      Primary Target IC<sub>50</sub>510 nM and 330 nM
      Primary Target K<sub>i</sub>310 nM and 140 nM, against ERK1 and ERK2, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      328007 0