Prinaberel

SKU: orb2900175

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.

Key Properties

• CAS Number: 524684-52-4
• MW: 271.24
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₀FNO₃
• SMILES: Oc1cc(C=C)c2oc(nc2c1)-c1ccc(O)c(F)c1
• Target: Estrogen Receptor/ERR
• Solubility: In Vitro: DMSO : ≥ 40 mg/mL (147.47 mM)

Bioactivity

• 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. 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. Animal model: Six-to eight-weeks-old SKH-1 hairless female mice. Dosage: 2 mg/mouse in 200μl ethanol. Administration: Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks. Result: Diminished UVB-induced skin tumor development in SKH-1 hairless mice.
• 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. 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. Prinaberel (0.01-10 μM) inhibits cell proliferation in a dose- and time-dependent manner. Prinaberel (10 μM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis. Western blot analysis. Cell line: A431 cells. Concentration: 0, 20, 40 and 60 μM. Incubation time: 24 hours. Result: Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.Cell Proliferation Assay Cell line: SKOV-3, A2780CP or OVCAR-3 cells. Concentration: 0.01, 0.1 and 10 μM Incubation time: 24-48 hours. Result: Showed significantly inhibitory effect on cell proliferation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR