Prinaberel (ERB-041) serves as a potent and selective agonist of estrogen receptor (ER) β, with IC50 values of 5.4, 3.1, and 3.7 nM for human, rat, and mouse ERβ, respectively. Prinaberel exhibits over 200-fold selectivity for ERβ over ERα. Furthermore, it acts as a potent chemopreventive agent for skin cancer by suppressing the WNT/β-catenin signaling pathway and inducing apoptosis in ovarian cancer cells[1][2][3].
体内研究
Topical application of Prinaberel at a dose of 2 mg/mouse, 30 minutes prior to UVB irradiation for 30 weeks, suppresses the development of squamous cell carcinoma in SKH-1 hairless mice[2].
Prinaberel exhibits a reduction in proliferation and angiogenesis, along with the induction of apoptosis in UVB-induced skin tumors. It also suppresses pro-inflammatory signaling pathways and diminishes tumor invasiveness via the PI3K-AKT pathway and WNT signaling[2].
体外研究
Prinaberel (ERB-041) at concentrations ranging from 0 to 60 µM for 24 hours induces cell differentiation, cell cycle arrest, and reduces colony formation in human squamous cell carcinoma (SCC) cells[2].
Prinaberel demonstrates a notable decrease in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS, and COX-2 in A431 cells. It also diminishes phosphorylated-PI3K and -AKT levels, leading to enhanced E-cadherin expression and reduced migration of A431 cells[2].
Prinaberel, at concentrations ranging from 0.01 to 10 µM, inhibits cell proliferation in a manner dependent on both dosage and time[3].
At a concentration of 10 µM for 48 hours, Prinaberel promotes apoptosis in ovarian cancer cells (SKOV-3 cells)[3].
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