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-κB 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].
In Vivo, PTPRO-IN-1 (Compound 30k) (20 mg/kg; p.o.; once daily for 10 consecutive days) exerts significant therapeutic effects in a DSS -induced mouse colitis model[1].
In Vitro, PTPRO-IN-1 (Compound 30k) (5 μM; 30 h) dose-dependently inhibits LPS -induced p-p65 expression and IL-6 secretion, as well as upregulation of TLR4 and phosphorylation of IKKα/β, in murine RAW264.7 and human THP-1 cells[1].
References:
[1]. Liang X, et al. Discovery of Benzofuran-2-Carboxylic Acid Derivatives as Potent PTPRO Inhibitors with Oral Efficacy for Treatment of Inflammatory Bowel Disease. J Med Chem. 2026;69(9):11167-11191.
In Vivo, PTPRO-IN-1 (Compound 30k) (20 mg/kg; p.o.; once daily for 10 consecutive days) exerts significant therapeutic effects in a DSS -induced mouse colitis model[1].
In Vitro, PTPRO-IN-1 (Compound 30k) (5 μM; 30 h) dose-dependently inhibits LPS -induced p-p65 expression and IL-6 secretion, as well as upregulation of TLR4 and phosphorylation of IKKα/β, in murine RAW264.7 and human THP-1 cells[1].
References:
[1]. Liang X, et al. Discovery of Benzofuran-2-Carboxylic Acid Derivatives as Potent PTPRO Inhibitors with Oral Efficacy for Treatment of Inflammatory Bowel Disease. J Med Chem. 2026;69(9):11167-11191.