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Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $33 | In Stock | |
5 mg | $84 | In Stock | |
1 mL x 10 mM (in DMSO) | $100 | In Stock |
Description | Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis. |
Targets&IC50 | ERα (rat):620 nM (IC50), ERβ (mouse):3.7 nM (IC50), ERα (mouse):750 nM (IC50), ERα (human):1200 nM (IC50), ERβ (human):5.4 nM (IC50), ERβ (rat):3.1 nM (IC50) |
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. [2] 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). [3] |
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. [2] |
Alias | WAY-202041, WAY202041, ERB041, ERB 041 |
Molecular Weight | 271.24 |
Formula | C15H10FNO3 |
Cas No. | 524684-52-4 |
Smiles | FC=1C=C(C=CC1O)C2=NC3=CC(O)=CC(C=C)=C3O2 |
Relative Density. | 1.31g/cm3 |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (110.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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