538770 GAK Inhibitor - Calbiochem

538770
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₂₁N₃O₄S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38770.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable isothiazolopyridine based compound that acts as a high-affinity binding, reversible and ATP-competitive inhibitor of cyclin G associated kinase (GAK; Kd = 8.3 nM). Displays moderate to excellent selectivity over Kit, PDGFRβ, Flt3, Mek5 & PDGFRα (Kd = 29, 70, 110, 150 & 220 nM, respectively) in a 456-kinase profiling. Shown to dose-dependently disrupt both HCV entry & assembly and efficiently arrest HCV infection (EC50 = 2.55 & 3.6 µM in HCVcc- & HCVpp-infected Huh-7.5 cells, respectively; CC50 = 23.27 µM in HCVcc-infected Huh-7.5 cells). Significantly inhibits intracellular & extracellular infectivity (EC50 = 1.64 & 2.13 µM, respectively) and AP2M1 phosphorylation. Exerts no effect on HCV RNA replication.
          Catalogue Number538770
          Brand Family Calbiochem®
          SynonymsCyclin G Associated Kinase Inhibitor, Auxilin 2 Inhibitor
          References
          ReferencesKovackova, S., et al. 2015. J. Med. Chem. 58, 3393.
          Product Information
          FormYellow solid
          Hill FormulaC₁₉H₂₁N₃O₄S
          Chemical formulaC₁₉H₂₁N₃O₄S
          ReversibleY
          Applications
          Biological Information
          Primary TargetGAK
          Secondary targetKit, PDGFRβ, Flt3, Mek5 & PDGFRα
          Purity≥98% 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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          GAK Inhibitor - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Kovackova, S., et al. 2015. J. Med. Chem. 58, 3393.
          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.

          Revision28-July-2017 JSW
          SynonymsCyclin G Associated Kinase Inhibitor, Auxilin 2 Inhibitor
          DescriptionA cell-permeable isothiazolopyridine based compound that acts as a high-affinity binding, reversible and ATP-competitive inhibitor of cyclin G associated kinase (GAK; Kd = 8.3 nM). Displays moderate to excellent selectivity over Kit, PDGFRβ, Flt3, Mek5 & PDGFRα (Kd = 29, 70, 110, 150 & 220 nM, respectively) in a 456-kinase profiling. Shown to dose-dependently disrupt both HCV entry & assembly and efficiently arrest HCV infection (EC50 = 2.55 & 3.6 µM in HCVcc- & HCVpp-infected Huh-7.5 cells, respectively; CC50 = 23.27 µM in HCVcc-infected Huh-7.5 cells). Significantly inhibits intracellular & extracellular infectivity (EC50 = 1.64 & 2.13 µM, respectively) and AP2M1 phosphorylation. Exerts no effect on HCV RNA replication.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₉H₂₁N₃O₄S
          Purity≥98% by HPLC
          SolubilityDMSO (50 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesKovackova, S., et al. 2015. J. Med. Chem. 58, 3393.