SW 033291

SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.IC50 value: 0.1 nM(Ki) [1]Target: 15-PGDHin vitro: SW033291 inhibition of 15-PGDH was noncompetitive versus PGE2 over concentrations up to 40 μM PGE2. SW033291 also demonstrated selective high-affinity interaction with 15-PGDH in thermal denaturation assays. Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with 50% of maximal stimulation (EC50) at ~75 nM [1].in vivo: mice injected with SW033291 closely phenocopied 15-PGDH knockout mice, with 10 mg per kg of weight (mg/kg) SW033291 inducing a twofold increase in PGE2 levels in bone marrow, colon, lung, and liver. Mice injected with SW033291 at 20 mg/kg daily for 7 days showed equivalent daily weights and activity as mice injected with vehicle-control and showed no adverse changes in blood counts or serum chemistry [1].

Signaling Pathways >> Metabolic Enzyme/Protease >> 15-PGDH

Research Areas >> Others

[1]. Zhang Y, et al. TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015 Jun 12;348(6240):aaa2340.