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

401480
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₄H₁₇N₅•2CF₃CO₂H 445430-58-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      401480-1MG
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          Plastic ampoule 1 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.