Estrogen receptor agonists and antagonists...low cost, high quality
Estrogen modulates many cellular processes including growth, differentiation and function of the reproductive system. Estrogen receptors include:
- estrogen receptors ERα and ERβ, which are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Both receptors interact with the same DNA response element and have a similar pharmacological profile.
- estrogen-related receptors (ERRs): ERRα, ERRβ and ERRγ. These are activated by co-regulatory proteins and bind the ERE and ERR response elements (ERREs) as homodimers, exerting transcriptional control of energy homeostasis.
- the G protein-coupled estrogen receptor (GPER, GPR30) which is a seven transmembrane spanning receptor that couples to heterotrimeric Gs-proteins. It functions independently from ERα or ERβ estrogen receptors. The GPER binds estradiol with high affinity, but has lower affinity for estrone and estriol.
As a specialist supplier of affordable estrogen receptor research tools, Hello Bio has introduced a range of low cost agonists and antagonists for estrogen receptors - at prices up to 50% less than other suppliers. Our range includes tools such as ICI 182780, an estrogen receptor (ER) antagonist and high affinity GPER agonist, and tamoxifen citrate. ERα selective tools include ERα agonist PPT. Our range of ERβ selective ligands include ERβ agonist DPN and ERβ antagonist PHTPP.
Browse our full range of estrogen receptor agonists and antagonists below:
Our prices are up to 50% less than other suppliers (check our price comparison table). However, we know that product reliability is more important than price. We are based in purpose built labs in the UK and with decades of synthetic and manufacturing chemistry expertise we know what we are doing! For your peace of mind, all of our products are covered by the Hello BioPromise quality guarantee.
Featured estrogen receptor and signaling products
A potent estrogen receptor (ER) antagonist (Ki values are = 1 and 3.6 nM at ERα and ERβ respectively). Shows no agonist activity and is devoid of estrogenic activity. Also a high affinity agonist at GPER (GPR30). Down-regulates the ER and impairs nuclear shuttling and dimerization of the receptor. Shows anticancer activity and active in vivo.. Find out more…DPN - selective ERβ agonist
Selective ERβ estrogen receptor agonist (Kd values are 5 and 400 nM at ERβ and ERα respectively). Shows 70-fold selectivity at ERβ over ERα. Shows neuroprotective effects. Active in vivo. Find out more
Cmpd101 is a novel, potent and selective G-protein coupled receptor kinase 2 and 3 (GRK2/GRK3) inhibitor (IC50 values are 35, 290 nM and 125 µM at GRK2, GRK3 and GRK5 respectively). It shows little activity at a broad range of other kinases. Membrane permeable, it can be used to study the roles of GRK2/3 in GPCR desensitization and other functions. Find out more…
Selective and reversible ATP-competitive c-Jun N-terminal Kinase (JNK) inhibitor (IC50 values are 40-90 µM at JNK1,2,3). Shows selectivity over a range of other kinases. Dose-dependently inhibits JNK phosphorylation and inhibits gene expression of COX-2, IL-2, IFN-γ and TNF-α. Prevents BMP9-induced osteogenic mesenchymal stem cell (MSC) differentiation. Active in vivo. Find out more...