Name | SW033291 |
Description | SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues. |
Kinase Assay | 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). |
In vitro | In Vaco-503 cells, SW033291 (2.5 μM) decreases cellular 15-PGDH enzyme activity by 85%.[1] |
In vivo | 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] |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 41.3 mg/mL (100 mM) Ethanol : 8.3 mg/mL (20 mM)
|
Keywords | knockout | PGE2 | 15-PGDH | Peripheral | prostaglandin | bone | SW033291 | inhibit | neutrophil | SW-033291 | SW 033291 | hematopoietic | 15-Hydroxyprostaglandin dehydrogenase | marrow | Inhibitor |
Inhibitors Related | Disulfiram | Methotrexate | ALDH1A3-IN-3 | Rotenone | Mycophenolate Mofetil | Ribavirin | 4-Diethylaminobenzaldehyde | Benzyl alcohol | Isomalt | Isoniazid | Sodium Oxamate | Ivosidenib |
Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |