Estrogen Receptors

Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.

(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.

GSK-1292263 is a novel GPR119 agonist.

GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ

GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.

Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.

Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist.

Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.

ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.

Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.

WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.

PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).

DY131(GSK 9089) is a novel selective agonist of ERRα and ERRβ.

Hexestrol is a carcinogenic synthetic estrogen that inhibits microtubule polymerization and the formation of ribbon structures. It is an inhibitor of lipid peroxidation.

LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM.

Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.

SLU-PP-332 is a pan-Estrogen Receptor/ERR agonist with EC50 values of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, respectively. SLUPP-332 enhances mitochondrial function and cellular respiration in skeletal muscle cell lines. SLU-PP-332 has the potential to study metabolic diseases as well as improve muscle function.