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401480 IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem

401480
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Overview

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Key Spec Table

CAS #Empirical Formula
445430-58-0C₁₄H₁₇N₅•2CF₃CO₂H

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      Description
      OverviewA cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
      Catalogue Number401480
      Brand Family Calbiochem®
      Synonyms4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
      References
      ReferencesTownsend, R.M., et al. 2004. Transplantation 77, 1090.
      MacMaster, J.F., et al. 2003. Inflamm. Res. 52, 508.
      McIntyre, K.W., et al. 2003. Arthritis Rheum. 48, 2652.
      Burke, J. R., et al. 2003. J. Biol. Chem. 278, 1450.
      Product Information
      CAS number445430-58-0
      ATP CompetitiveN
      FormOff-white solid
      FormulationSupplied as bis-TFA salt.
      Hill FormulaC₁₄H₁₇N₅•2CF₃CO₂H
      Chemical formulaC₁₄H₁₇N₅•2CF₃CO₂H
      Hygroscopic Hygroscopic
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetIKK-2
      Primary Target IC<sub>50</sub>~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells
      Purity≥96% 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
      Hygroscopic Hygroscopic
      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

      IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      401480

      References

      Reference overview
      Townsend, R.M., et al. 2004. Transplantation 77, 1090.
      MacMaster, J.F., et al. 2003. Inflamm. Res. 52, 508.
      McIntyre, K.W., et al. 2003. Arthritis Rheum. 48, 2652.
      Burke, J. R., et al. 2003. J. Biol. Chem. 278, 1450.
      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-April-2011 RFH
      Synonyms4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
      DescriptionA cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
      FormOff-white solid
      FormulationSupplied as bis-TFA salt.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number445430-58-0
      Chemical formulaC₁₄H₁₇N₅•2CF₃CO₂H
      Structure formulaStructure formula
      Purity≥96% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      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 Standard Handling
      ReferencesTownsend, R.M., et al. 2004. Transplantation 77, 1090.
      MacMaster, J.F., et al. 2003. Inflamm. Res. 52, 508.
      McIntyre, K.W., et al. 2003. Arthritis Rheum. 48, 2652.
      Burke, J. R., et al. 2003. J. Biol. Chem. 278, 1450.