Prinaberel

SKU: orb1679034

Description

Prinaberel (ERB-041) is a potent and selective ERβ agonist that demonstrates anticancer and anti-inflammatory activity. It has been studied in models of endometriosis, where its ability to inhibit NF-κB signaling, reduce proliferation, and induce apoptosis has been investigated in both in vitro and in vivo experimental settings.

Research Area

Cell Biology, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 524684-52-4
• MW: 271.24
• Formula: C₁₅H₁₀FNO₃
• SMILES: FC=1C=C(C=CC1O)C2=NC3=CC(O)=CC(C=C)=C3O2
• Target: Wnt/beta-catenin|||Apoptosis|||Estrogen/progestogen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (18.43 mM);DMSO:30 mg/mL (110.6 mM)

Bioactivity

• Target IC50:
  ERβ (rat):3.1 nM (IC50)|ERα (mouse):750 nM (IC50)|ERβ (human):5.4 nM (IC50)|ERα (human):1200 nM (IC50)|ERβ (mouse):3.7 nM (IC50)|ERα (rat):620 nM (IC50)
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• In Vivo:
  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.
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• In Vitro:
  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. 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).
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Storage & Handling

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

Alternative Names

Estrogen Receptor, EstrogenReceptor, ERβ, ERB 041, ERB041, ERB-041, betacatenin, beta-catenin, bcatenin, apoptosis, βcatenin, progestogen Receptor, progestogenReceptor, WAY202041, WAY-202041, Prinaberel, Wnt/betacatenin, Wnt/b-catenin, WNT, Wnt, Wnt/β-catenin

Compound Identifiers

PubChem CID

656954