SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.

15-PGDH:0.1 nM(Ki), 15-PGDH:1.5 nM

In Vaco-503 cells, SW033291 (2.5 μM) decreases cellular 15-PGDH enzyme activity by 85%.[1]

In mice receiving a bone marrow transplant, SW033291 (10 mg/kg, i.p.) promotes hematopoietic recovery. In mouse models of colon and liver injury, SW033291 (10 mg/kg, i.p.) reduces the levels of colitis-associated inflammatory cytokines, protects mice from colitis, and promotes liver regeneration. [1]

Fluorescence anisotropy (FP) ligand displacement assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM).