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15-PGDH (15-Hydroxyprostaglandin dehydrogenase) is a tumor suppressor in breast, colon, liver, lung, and pancreas since decreased expression of this enzyme is associated with increased tumorigenesis. 15-PGDH metabolizes intracellular PGE2 so that this ligand is unable to bind EP receptors, which results in suppression of PGE2 signaling.
The tumor suppressor 15-PGDH is the key enzyme in prostaglandin E2 catabolism and is down-regulated in colorectal cancer (CRC) tissue. Canonical Wnt signaling is frequently elevated in colon cancers and has been shown to down-regulate 15-PGDH expression.
Inhibition of 15-PGDH, a prostaglandin-degrading enzyme, potentiates tissue regeneration in multiple organs in mice. 15-PGDH acts in vivo as a negative regulator of prostaglandin levels and activity, provides a candidate target.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
GY04204 |
SW033291 |
459147-39-8 | A potent and selective inhibitor of 15-PGDH with Ki of 0.1 nM, IC50 of 1.5 nM; increases PGE2 levels by 3.5-fold at 500 nM, with EC50 of 75 nM; increases prostaglandin PGE2 levels in bone marrow and other tissues, accelerates hematopoietic recovery in mice receiving a bone marrow transplant; also promotes tissue regeneration in mouse models of colon and liver injury. |
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