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506172 p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₃₁H₃₇N₅O₃ 285983-48-4

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506172-10MG
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      Description
      OverviewA cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
      Catalogue Number506172
      Brand Family Calbiochem®
      Synonyms1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII, Doramapimod, BIRB796
      References
      ReferencesLiu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
      Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
      Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
      Regan, J., et al. 2002. J. Med. Chem. 45, 2994.
      Product Information
      CAS number285983-48-4
      FormWhite solid
      Hill FormulaC₃₁H₃₇N₅O₃
      Chemical formulaC₃₁H₃₇N₅O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Applicationp38 MAP Kinase Inhibitor X, BIRB 796, CAS 285983-48-4, is a cell-permeable, highly potent, slow binding, high affinity inhibitor of p38a (IC50 = 8 and 97 nM with or without 2 h preincubation).
      Biological Information
      Purity≥99% by HPLC
      Physicochemical Information
      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 Regulatory Review
      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

      Documentation

      p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      p38 MAP Kinase Inhibitor X, BIRB 796 - CAS 285983-48-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      506172

      References

      Reference overview
      Liu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
      Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
      Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
      Regan, J., et al. 2002. J. Med. Chem. 45, 2994.
      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.

      Revision02-October-2012 JSW
      Synonyms1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII, Doramapimod, BIRB796
      DescriptionA cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production in cultures in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84% and 63%, respectively, with oral dosage of 30 mg/kg and 10 mg/kg).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number285983-48-4
      Chemical formulaC₃₁H₃₇N₅O₃
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml; clear, colorless 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 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesLiu. Y. and Gray, N.S., 2006. Nat. Chem. Biol. 2, 358.
      Regan, J., et al. 2003. J. Med. Chem. 46, 4676.
      Pargellis, C., et al. 2002. Nat. Struct. Biol. 9, 268.
      Regan, J., et al. 2002. J. Med. Chem. 45, 2994.