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

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420150-10MG
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          Glass bottle 10 mg
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          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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