Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
性状
Solid
IC50 & Target[1][2]
IC50: 26 nM (ERα), 99 nM (ERβ)
体外研究(In Vitro)
Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6.
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line:
AsPC-1 cells
Concentration:
10 μM, 20 μM
Incubation Time:
2 hours
Result:
Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.