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MedChemExpress - Model Prinaberel - ...

MedChemExpress - Model Prinaberel - 524684-52-4

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].

Prinaberel

MCE China：Prinaberel

Brand：MedChemExpress (MCE)

Cat. No.HY-14933

CAS：524684-52-4

Synonyms：ERB-041

Purity：98.05%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：hERβ 5.4 nM (IC50) rat ERβ 3.1 nM (IC50) mouse ERβ 3.7 nM (IC50) hERα 1200 nM (IC50) mouse ERα 750 nM (IC50) rat ERα 620 nM (IC50)

References：

[1]. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040. [Content Brief]

[2]. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014;7(2):186-198. [Content Brief]

[3]. Chan KKL, et al. Estrogen receptor modulators genistein, daidzein and ERB-041 inhibit cell migration, invasion, proliferation and sphere formation via modulation of FAK and PI3K/AKT signaling in ovarian cancer. Cancer Cell Int. 2018;18:65. Published 2018 May 1. [Content Brief]

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