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420149 | JNK Inhibitor XV, IQ-1S - Calbiochem

420149
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₈N₃Ona

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420149-25MG
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      Stocked 
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      Available
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable indenoquinoxalinone-oxime (IQ) compound that acts as a potent, non-toxic, reversible, ATP-competitive, high-affinity inhibitor of JNK (Kd = 390, 360 and 87 nM for JNK1, JNK2 and JNK3, respectively) with moderate selectivity over CK1δ, PI 3-Kγ, and MKNK2 (IC50 = 1.4, 1.2, and 1.8 µM, respectively). Shown to reduce c-Jun-Ser63 phosphorylation, and block the production of LPS-induced TNF-α (IC50 = 250 nM) and IL-6 (IC50 = 610 nM) in MonoMac-6 monocytic cells and in human hPBMCs, respectively. Also shown to inhibit NF-κB/AP-1 reporter activity (IC50 = 1.8 µM) in human THP1-Blue monocytic cells and diminish nitric oxide production in murine J774-A.1 macrophages (IC50 = 12.5 µM). Exhibits favorable pharmacokinetics properties and efficiently reduces ovalbumin-induced CD+ T-cell immune inflammation in a murine delayed-type hypersensitivity model (12.5 mg/kg, two per day dosage, i.p.).
          Catalogue Number420149
          Brand Family Calbiochem®
          Synonyms11H-Indeno[1,2-b]quinoxalin-11-one oxime, sodium salt
          References
          ReferencesSchepetkin, I.A., et al. 2012. Mol. Pharmacol. 81, 832.
          Product Information
          FormBright yellow solid
          Hill FormulaC₁₅H₈N₃Ona
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula Image
          Applications
          Biological Information
          Primary TargetJNK1,2,3
          Secondary targetPI 3-Kγ, CK1δ and MKNK2
          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 -20°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
          420149

          References

          Reference overview
          Schepetkin, I.A., et al. 2012. Mol. Pharmacol. 81, 832.
          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.

          Revision24-August-2012 JSW
          Synonyms11H-Indeno[1,2-b]quinoxalin-11-one oxime, sodium salt
          DescriptionA cell-permeable indenoquinoxalinone-oxime (IQ) compound that acts as a potent, non-toxic, reversible, ATP-competitive, high-affinity inhibitor of JNK (Kd = 390, 360 and 87 nM for JNK1, JNK2 and JNK3, respectively) with moderate selectivity over CK1δ, PI 3-Kγ, and MKNK2 (IC50 = 1.4, 1.2, and 1.8 µM, respectively). Shown to reduce c-Jun-Ser63 phosphorylation, and block the production of LPS-induced TNF-α (IC50 = 250 nM) and IL-6 (IC50 = 610 nM) in MonoMac-6 monocytic cells and in human hPBMCs, respectively. Also shown to inhibit NF-κB/AP-1 reporter activity (IC50 = 1.8 µM) in human THP1-Blue monocytic cells and diminish nitric oxide production in murine J774-A.1 macrophages (IC50 = 12.5 µM). Exhibits favorable pharmacokinetics properties and efficiently reduces ovalbumin-induced CD+ T-cell immune inflammation in a murine delayed-type hypersensitivity model (12.5 mg/kg, two per day dosage, i.p.).
          FormBright yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Structure formula
          Purity≥95% by HPLC
          SolubilityDMSO (10 mg/ml)
          Storage -20°C
          Protect from light
          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.
          Toxicity Standard Handling
          ReferencesSchepetkin, I.A., et al. 2012. Mol. Pharmacol. 81, 832.