Cat. No. 1991
Chemical Name: 1,3-Bis(4-hydroxyphenyl)-4-methyl-5
Biological ActivitySelective, high affinity silent antagonist at ERα receptors. Displays > 200-fold selectivity for ERα over ERβ. Ki values are 2.7 and 1800 nM at ERα and ERβ receptors respectively.
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
Harrington et al (2003) Activities of estrogen receptor alpha- and beta-selective ligands at diverse responsive gene sites mediating transactivation or transrepression. Mol.Cell.Endocrinol. 206 13. PMID: 12943986.
Sun et al (2002) Antagonists selective for estrogen receptor α. Endocrinol. 143 941.
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Citations are publications that use Tocris products. Selected citations for MPP dihydrochloride include:
Wang et al (2015) Bu-Shen-Ning-Xin decoction: inhibition of osteoclastogenesis by abrogation of the RANKL-induced NFATc1 and NF-κB signaling pathways via selective estrogen receptor α. Drug Des Devel Ther 9 3755. PMID: 26229438.
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.
Cruz et al (2013) High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses. PLoS Negl Trop Dis 7 e2073. PMID: 23437413.
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.
Lam et al (2012) Phosphorylation of human estrogen receptor-beta at serine 105 inhibits breast cancer cell migration and invasion. Mol Cell Endocrinol 358 27. PMID: 22370157.
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Keywords: MPP dihydrochloride, supplier, selective, Erα, receptor, antagonist;, ERalpha, antagonists, ER, ERR, Estrogen, Receptors, Tocris Bioscience, Estrogen and Related Receptor Antagonist products
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