Cat. No. 2662
Chemical Name: 4-[2-Phenyl-5,7-bis(trifluoromethyl
Biological ActivitySelective estrogen ERβ receptor antagonist that displays 36-fold selectivity over ERα. Exhibits full antagonism at ERβ in a cotransfection assay in human endometrial cancer cells (HEC-1), with minimal effects on ERα.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Compton et al (2005) Erratum. J.Med.Chem. 48 2724.
Compton et al (2004) Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity. J.Med.Chem. 47 5872. PMID: 15537344.
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Citations are publications that use Tocris products. Selected citations for PHTPP include:
Hamilton et al (2015) Biologic roles of estrogen receptor-β and insulin-like growth factor-2 in triple-negative breast cancer. Biomed Res Int 2015 925703. PMID: 25874233.
Harvey et al (2015) Methoxychlor and its metabolite HPTE inhibit cAMP production and expression of estrogen receptors α and β in the rat granulosa cell in vitro. Reprod Toxicol 51 72. PMID: 25549949.
Gorelick et al (2014) Transgenic zebrafish reveal tissue-specific differences in estrogen signaling in response to environmental water samples. Environ Health Perspect 122 356. PMID: 24425189.
Koong and Watson (2014) Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589. PMID: 25213831.
Ogo et al (2014) IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells. J Reprod Dev 60 216. PMID: 24670778.
Kim et al (2013) Effects of 17β-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell lines. J Gastric Cancer 13 172. PMID: 24156037.
Samanta et al (2012) Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer. Oncogene 31 4689. PMID: 22266872.
Simpkins et al (2012) Src Inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo. Clin Cancer Res 18 5911. PMID: 22896656.
Ivanova et al (2011) Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites. FASEB J 25 1402. PMID: 21233487.
Aguirre et al (2010) Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β. J Neurochem 115 1277. PMID: 20977477.
Weiser et al (2009) Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress. Endocrinology 150 1817. PMID: 19074580.
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Keywords: PHTPP, supplier, Selective, ERβ, ERbeta, antagonists, Estrogen, Receptors, Tocris Bioscience, Estrogen and Related Receptor Antagonist products
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