538770 GAK Inhibitor - Calbiochem

538770
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₉H₂₁N₃O₄S

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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
      Quality LevelMQ100
      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.