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538770 GAK Inhibitor - Calbiochem

GAK Inhibitor - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Cyclin G Associated Kinase Inhibitor, Auxilin 2 Inhibitor

Primary Target: GAK
538770
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Přehled

Replacement Information

Tabulka spec. kláve

Empirical Formula
C₁₉H₂₁N₃O₄S

Products

Katalogové čísloBalení ks/bal.
5.38770.0001 Skleněná láhev 10 mg
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
Global Trade Item Number
Katalogové číslo GTIN
5.38770.0001 04054839119729

Documentation

GAK Inhibitor - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
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 Protect from light
+2°C to +8°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 Standard Handling
ReferencesKovackova, S., et al. 2015. J. Med. Chem. 58, 3393.