| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| Name | Prinaberel | ||||||||||||
| CAS | 524684-52-4 | ||||||||||||
| Formula | C15H10FNO3 | ||||||||||||
| Molar Mass | 271.24 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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