5.38770
GAK Inhibitor
Synonym(s):
GAK Inhibitor, Cyclin G Associated Kinase Inhibitor, Auxilin 2 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C19H21N3O4S
Molecular Weight:
387.45
NACRES:
NA.77
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
Related Categories
Biochem/physiol Actions
Cell permeable: yes
Primary Target
GAK
GAK
Reversible: yes
Secondary Target
Kit, PDGFRβ, Flt3, Mek5 & PDGFRα
Kit, PDGFRβ, Flt3, Mek5 & PDGFRα
Disclaimer
Toxicity: Standard Handling (A)
General description
A 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.
Other Notes
Kovackova, S., et al. 2015. J. Med. Chem.58, 3393.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 5.38770.0001 | 04054839119729 |
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