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506385 p38 MAP Kinase Inhibitor XX, MW108 - CAS 1628503-09-2 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Primary Target: p38a MAPK
506385
  
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      Overview

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      1628503-09-2C₂₁H₁₈N₄•2HCl
      Description
      Overview

      This product has been discontinued.



      A cell-permeable, aminopyridazine derivative that acts as a highly selective, active site targeted, and stable inhibitor of neuronal p38 alpha MAP Kinase (Ki = 114 nM) and exhibit about 10-fold greater selectivity over casein kinase 1d (IC50 > 1 µM). Does not exhibit any significant inhibitory activity against a panel of 290 protein kinases. Exhibits desirable aqueous solubility and blood-brain barrier permeability. Binds to human p38 alpha with DFG-in conformation, but without inducing a glycine flip conformational change. Reduces lipopolysaccharide and TLR-ligand-induced overproduction of IL-1b (IC50 = 610 nM). Also shown to ameliorate Aβ42-induced memory impairment and improve synaptic functions in mice (~ 5 mg/kg, i.p).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number506385
      Brand Family Calbiochem®
      References
      ReferencesWatterson, D.M., et al. 2013.PLos One. 8, e66226.
      Product Information
      CAS number1628503-09-2
      FormYellow solid
      Hill FormulaC₂₁H₁₈N₄•2HCl
      Chemical formulaC₂₁H₁₈N₄•2HCl
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetp38a MAPK
      Primary Target K<sub>i</sub>114 nM
      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 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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      506385 0

      Documentation

      p38 MAP Kinase Inhibitor XX, MW108 - CAS 1628503-09-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Watterson, D.M., et al. 2013.PLos One. 8, e66226.
      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.

      Revision31-July-2014 JSW
      DescriptionA cell-permeable, aminopyridazine derivative that acts as a highly selective, active site targeted, and stable inhibitor of neuronal p38 alpha MAP Kinase (Ki = 114 nM) and exhibit about 10-fold greater selectivity over casein kinase 1d (IC50 > 1 µM). Does not exhibit any significant inhibitory activity against a panel of 290 protein kinases. Exhibits desirable aqueous solubility and blood-brain barrier permeability. Binds to human p38 alpha with DFG-in conformation, but without inducing a glycine flip conformational change. Reduces lipopolysaccharide and TLR-ligand-induced overproduction of IL-1b (IC50 = 610 nM). Also shown to ameliorate Aβ42-induced memory impairment and improve synaptic functions in mice (~ 5 mg/kg, i.p).
      FormYellow solid
      CAS number1628503-09-2
      Chemical formulaC₂₁H₁₈N₄•2HCl
      Purity≥98% by HPLC
      SolubilityH₂O (100 mg/ml) or DMSO (100 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesWatterson, D.M., et al. 2013.PLos One. 8, e66226.