Bazedoxifene

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^[1][2]. IC50 & Target: IC50: 26 nM (ERα), 99 nM (ERβ)^[1] In Vitro: Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain^[1].
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling^[1].
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells^[2].
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells^[2].
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6^[2].
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130^[2].
In Vivo: Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo^[2].