15-PGDH | Biologically Active Compounds

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.

ML148

ML148 is a potent and selective 15-PGDH inhibitor with an IC50 of 56 nM. ML148 has the potential for the research of prostaglandin-signaling pathways[1].

CAS Number: 451496-96-1
MF: C₂₀H₂₁N₃O
MW: 319.40
Catalog: 15-PGDH

Density: 1.2±0.1 g/cm3
Boiling Point: 543.4±52.0 °C at 760 mmHg
Melting Point: N/A
Flash Point: 282.5±30.7 °C

Price

Suppliers

15-PGDH-IN-1

15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].

CAS Number: 2241676-74-2
MF: C₂₄H₂₂N₄O₂
MW: 398.46
Catalog: 15-PGDH

Density: N/A
Boiling Point: N/A
Melting Point: N/A
Flash Point: N/A

Price

Suppliers

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].

CAS Number: 459147-39-8
MF: C₂₁H₂₀N₂OS₃
MW: 412.591
Catalog: 15-PGDH

Density: 1.4±0.1 g/cm3
Boiling Point: 670.1±55.0 °C at 760 mmHg
Melting Point: N/A
Flash Point: 359.0±31.5 °C

Price

Suppliers