Cas No.: | 459147-39-8 |
Chemical Name: | 2-(butylsulfinyl)-6-(2,3-dihydrothiophen-2-yl)-4-phenylthieno[2,3-b]pyridin-3-amine |
Synonyms: | SW033291,SW-033291,SW033291,SW 033291 |
SMILES: | C12SC(S(CCCC)=O)=C(N)C1=C(C1=CC=CC=C1)C=C(C1SC=CC=1)N=2 |
Formula: | C21H22N2Os3 |
M.Wt: | 414.61 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |
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]. |
In 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]. |