MilliporeSigma™ Calbiochem™ sPLA2-IIA Inhibitor II, KH064

Description

• A reversible, potent, and selective sPLA2-IIA/PLA2g2a (phospholipase A2 group IIA) inhibitor (IC50 = 29nM) that displays much reduced potency against sPLA2-V/PLA2g5 (PLA2 group V; IC50 = 2μM) and is reported not to affect the activity of cytosolic cPLA2, Ca2+-independent iPLA2, 30 human GPCRs, and 25 other enzymes
• In addition to being useful in studying PLA2g2a-mediated cellular responses in cultures in vitro (100% inhibition of LPS-induced PGE2 production in HMC-1 cells; 15 min 10μM pretreatment), KH064 is orally available in rats and efficacious in various rat disease models in vivo (5mg/kg p.o.), including adjuvant-induced arthritis, spontaneous hypertension, high fat diet-induced metabolic disorders
• Comparing to the substrate-competitive inhibitor c(2NapA)LS(2NapA)R (Cat
• No
• 525145), KH064 also effectively chelates sPLA2-IIA active site Ca2+ in addition to targeting the enzyme's N-terminal lipid substrate binding site.