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

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Synonyme: 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine

Primary Target: ERK1 and ERK2
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      Übersicht

      Replacement Information

      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
      Applications
      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
      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 +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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      328007 0

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

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

      TitelChargennummer
      328007

      Literatur

      Übersicht
      Ohori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.

      Posters

      Titel
      Human Kinome & InhibitorSelect™ Libraries
      Datenblatt

      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.

      Revision16-January-2012 RFH
      Synonyms5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
      DescriptionA 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 of 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008). Also available in InSolution™ format (Cat. No. 328010).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number865362-74-9
      Chemical formulaC₁₈H₁₃N₇
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesOhori, M., et al. 2005. Biochem. Biophys. Res. Commun. 336, 357.