GK470
GK470 (compound 28) is an inhibitor of group IVA cytosolic phospholipase A2 (GIVA cPLA2) with an IC50 of 300 nM in vesicle assays. GK470 has anti-inflammatory activity, inhibiting the release of arachidonic acid in SW982 fibroblast-like synoviocytes with an IC50 value of 0.6 μM. GK470 exhibits comparable anti-inflammatory effects to Methotrexate in a preventive collagen-induced arthritis model and significantly reduces plasma PGE2 levels[1].
Product Specifications
CAS Number
1621517-53-0
UNSPSC
12352005
Target
Phospholipase
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/gk470.html
Smiles
O=C(OC)C1=CSC(C(COC2=CC=C(C=C2)CCCCCCCC)=O)=N1
Molecular Formula
C21H27NO4S
Molecular Weight
389.51
References & Citations
[1]Kokotos G, et al. Inhibition of group IVA cytosolic phospholipase A2 by thiazolyl ketones in vitro, ex vivo, and in vivo[J]. Journal of medicinal chemistry, 2014, 57 (18) : 7523-7535.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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