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401481 IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₂H₁₀FN₃O₂S 507475-17-4

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401481-500UG
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      Plastic ampoule 500 μg
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      Description
      OverviewA cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). A 10 mM (500 µg/179 µl) solution of IKK-2 Inhibitor IV (Cat. No. 401484) in DMSO is available.
      Catalogue Number401481
      Brand Family Calbiochem®
      Synonyms[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
      References
      ReferencesPodolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
      Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
      Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.
      Product Information
      CAS number507475-17-4
      ATP CompetitiveY
      FormPale yellow solid
      Hill FormulaC₁₂H₁₀FN₃O₂S
      Chemical formulaC₁₂H₁₀FN₃O₂S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetIKK-2
      Primary Target IC<sub>50</sub>18 nM against IKK-2
      Purity≥95% 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
      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-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      401481

      References

      Reference overview
      Podolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
      Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
      Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.
      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.

      Revision18-January-2010 RFH
      Synonyms[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
      DescriptionA cell-permeable, reversible, ATP-competitive, and potent inhibitor of IKK-2 (IC50 = 18 nM) that exhibits selectivity over IKK-1, JNK, and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Shown to reduce paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number507475-17-4
      Chemical formulaC₁₂H₁₀FN₃O₂S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      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 Standard Handling
      ReferencesPodolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
      Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
      Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.