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 / Product Datasheet / 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:
Xing et al (2016) Direct Regulation of Aromatase B Expression by 17β-Estradiol and Dopamine D1 Receptor Agonist in Adult Radial Glial Cells. Cell Death Differ 9 504. PMID: 26793050.
Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. J Biol Chem 6 894. PMID: 26441850.
Gao et al (2015) Rapid responses and mechanism of action for low-dose bisphenol S on ex vivo rat hearts and isolated myocytes: evidence of female-specific proarrhythmic effects. Front Neurosci 123 571. PMID: 25723814.
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.
Vinnedge et al (2012) The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer. Front Microbiol 7 e46985. PMID: 23071688.
Chan et al (2010) Activation of GPR30 inhibits the growth of prostate cancer cells through sustained activation of Erk1/2, c-jun/c-fos-dependent upregulation of p21, and induction of G(2) cell-cycle arrest. Proc Natl Acad Sci U S A 17 1511. PMID: 20203690.
Dong et al (2006) A novel estradiol/estrogen receptor α-dependent transcriptional mechanism controls expression of the human prolactin receptor. Environ Health Perspect 281 18825. PMID: 16651265.
May et al (2006) Estrogens protect pancreatic β-cells from apoptosis and prevent insulin-deficient diabetes mellitus in mice. Neuropharmacology 103 9232. PMID: 16754860.
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