| Bioactivity | 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 (HY-14519) in a preventive collagen-induced arthritis model and significantly reduces plasma PGE2 levels[1]. |
| CAS | 1621517-53-0 |
| Formula | C21H27NO4S |
| Molar Mass | 389.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |