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401487 IKK-2 Inhibitor VIII - CAS 406208-42-2 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
406208-42-2C₂₁H₂₄N₄O₂

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401487-1MG
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      Description
      OverviewA cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC50 = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC50 >20 µM). Exhibits good aqueous solubility (0.12 mg/ml in pH 7.4 isotonic buffer) and potent activity in various cellular assays in vitro (IC50 <150 nM). Shown to be orally bioavailable both in rats and mice (BA = 60% and 16%, respectively) and effectively inhibit arachidonic acid-induced swelling in a murine ear edema model in vivo.
      Catalogue Number401487
      Brand Family Calbiochem®
      Synonyms2-Amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-(4-piperidinyl)-3-pyridinecarbonitrile, ACHP
      References
      ReferencesMurata, T., et al. 2004. Bioorg. Med. Chem. Lett. 14, 4019.
      Product Information
      CAS number406208-42-2
      ATP CompetitiveN
      FormYellow solid
      Hill FormulaC₂₁H₂₄N₄O₂
      Chemical formulaC₂₁H₂₄N₄O₂
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetIKK-2
      Primary Target IC<sub>50</sub>8.5 and 250 nM for IKK-2 and IKK-1, respectively
      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 Shipped with Blue Ice or with Dry Ice
      Toxicity Irritant
      Storage -20°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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      401487-1MG 04055977212044

      Documentation

      IKK-2 Inhibitor VIII - CAS 406208-42-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      IKK-2 Inhibitor VIII - CAS 406208-42-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      401487

      References

      Reference overview
      Murata, T., et al. 2004. Bioorg. Med. Chem. Lett. 14, 4019.

      Brochure

      Title
      Biologics 33.2
      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.

      Revision13-April-2011 RFH
      Synonyms2-Amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-(4-piperidinyl)-3-pyridinecarbonitrile, ACHP
      DescriptionA cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC50 = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC50 >20 µM). Exhibits good aqueous solubility (0.12 mg/ml in pH 7.4 isotonic buffer) and potent activity in various cellular assays in vitro (IC50 <150 nM). Shown to be orally bioavailable both in rats and mice (BA = 60% and 16%, respectively) and effectively inhibit arachidonic acid-induced swelling in a murine ear edema model in vivo.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number406208-42-2
      Chemical formulaC₂₁H₂₄N₄O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml). Sonication is required for complete solubilization.
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Irritant
      ReferencesMurata, T., et al. 2004. Bioorg. Med. Chem. Lett. 14, 4019.