420150 JNK Inhibitor XVI, JNK-IN-8 - Calbiochem

420150
  
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₉H₂₉N₇O₂ 1410880-22-6
      Description
      OverviewA cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys116 in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC50 = 486 nM in HeLa cells; 338 nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC50 = 92 nM for V559D and 56 nM for T670I) and RIOK2 (120 nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK.
      Catalogue Number420150
      Brand Family Calbiochem®
      Synonyms(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
      References
      ReferencesZhang, T., et al. 2011. Chem. Biol. 19, 140
      Product Information
      CAS number1410880-22-6
      DeclarationLicensed under pending patent from Dana-Farber Cancer Institute.
      FormLight yellow to yellow powder
      Hill FormulaC₂₉H₂₉N₇O₂
      Chemical formulaC₂₉H₂₉N₇O₂
      ReversibleN
      Structure formula ImageStructure formula Image
      Applications
      ApplicationJNK Inhibitor XVI, JNK-IN-8, CAS 1410880-22-6, is a cell-permeable, selective, irreversible type 2 inhibitor of c-Jun kinases (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, 2 & 3, respectively).
      Biological Information
      Primary TargetJNK1, JNK2, JNK3
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      JNK Inhibitor XVI, JNK-IN-8 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      JNK Inhibitor XVI, JNK-IN-8 - Calbiochem Certificates of Analysis

      TitleLot Number
      420150

      References

      Reference overview
      Zhang, T., et al. 2011. Chem. Biol. 19, 140
      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.

      Revision12-October-2016 JSW
      Synonyms(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
      DescriptionA cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys116 in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC50 = 486 nM in HeLa cells; 338 nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC50 = 92 nM for V559D and 56 nM for T670I) and RIOK2 (120 nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK.
      FormLight yellow to yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1410880-22-6
      Chemical formulaC₂₉H₂₉N₇O₂
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml; clear, yellowish solution)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesZhang, T., et al. 2011. Chem. Biol. 19, 140