Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.

ERα (rat):620 nM (IC50), ERβ (human):5.4 nM (IC50), ERα (human):1200 nM (IC50), ERβ (rat):3.1 nM (IC50), ERβ (mouse):3.7 nM (IC50), ERα (mouse):750 nM (IC50)

Treatment of human squamous cell carcinoma (SCC) cells with Prinaberel (0-60 µM for 24 h) promoted cell differentiation, blocked the cell cycle, and reduced cell colony formation. In A431 cells, Prinaberel significantly decreased the expression of inflammation-regulating proteins such as p-NFκBp65, iNOS, and COX-2. Prinaberel inhibited the phosphorylation levels of PI3K and AKT, as well as enhanced the expression of E-cadherin, and reduced the migration ability of A431 cells. [2]
Prinaberel (0.01-10 µM) inhibited cell proliferation in a dose- and time-dependent manner.Prinaberel (10 µM, 48 h) induced apoptosis in ovarian cancer cells (SKOV-3 cells). [3]

In the SKH-1 nude mouse model, Prinaberel (2 mg/mouse, topical application, 30 minutes prior to UVB irradiation, weekly for 30 weeks) inhibited the development of squamous cell carcinoma.Prinaberel inhibited cell proliferation and angiogenesis, while promoting apoptosis, in UVB-induced skin tumors.Prinaberel also inhibited UVB Prinaberel also inhibited the pro-inflammatory signaling pathway in UVB-induced skin tumors and reduced tumor invasiveness by modulating the PI3K-AKT pathway and the WNT signaling pathway. [2]