PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC50 of 0.16 µM. PTPRO-IN-1 exhibits IC50 values of 2.4 µM, 2.33 µM and 2.13 µM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-kappaB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease[1].