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

401481
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₁₀FN₃O₂S 507475-17-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          Biologics 32.3 PDF ( 927 KB )
          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.