This report describes the development of jasmonic acid biosynthesis inhibitor in our laboratory. We designed the jasmonic acid inhibitor targeting on the allene oxide synthase (AOS) and structure-activity relationships studies revealed a potent inhibitor, JM-8686, with an IC_<50> value of approximate 10nM in an in vitro assay. Kinetic analysis of JM-8686 indicated it was a competitive inhibitor of AOS. Stereochemical structure-activity relationship studies indicated that the potency of (R)-(-)-JM-8686 was about 200 times of that of (S)-(+)-JM-8686, with an IC_<50> value of approximate 5nM and 1,000nM, respectively.