ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), effectively targeting hGX with an IC50 of 80 nM. It efficiently inhibits the phosphorylation of ERK1/2 and p-38. sPLA2s, belonging to the disulfide-rich, Ca2+-dependent enzyme family, catalyze the hydrolysis of glycero-phospholipids at the sn-2 position, resulting in the release of a fatty acid and a lysophospholipid. ROC-0929 holds promise in researching inflammation-related diseases.