Prinaberel

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC₅₀s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis^[1][2][3]. In Vitro: Prinaberel (ERB-041) (0-60 μM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation^[2].
Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells^[2].
Prinaberel (0.01-10 μM) inhibits cell proliferation in a dose- and time-dependent manner^[3].
Prinaberel (10 μM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis^[3]. In Vivo: Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice^[2].
Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling^[2].