errγ

ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective, and orally bioavailable estrogen-related receptor gamma (ERRγ) inverse agonist with an IC50 of 40 nM [1].

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

DY131 (DY-131) is a novel selective agonist of ERRβ and ERRγ.

GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

ERRγ agonist-1 can be used in neuropsychological disorders research. ERRγ agonist-1 increases the ERRγ transcriptional activities that is a potent agonist of ERRγ [1].

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM, inhibiting the expression of hepcidin, fibrinogen, and gluconeogenic genes. ERRγ agonist-2 exhibits antimicrobial, anti-coagulant, and antidiabetic activities [1].

(E/Z)-GSK5182 (GSK5182(Z/E)) is a racemic mixture comprising (E)-GSK5182 and (Z)-GSK5182 isomers. It acts as a highly selective and orally active inverse agonist for the estrogen-related receptor γ (ERRγ), demonstrating potency with an IC50 of 79 nM. Additionally, GSK5182 is known to induce the generation of reactive oxygen species (ROS) in hepatocellular carcinoma.

SLU-PP-1072 is an ERRα and ERRγ inverse dual agonist that disrupts PCa cell metabolism and induces apoptosis through cell cycle dysregulation.SLU-PP-1072 is used to study prostate cancer (PCa).

SLU-PP-332 is a pan-estrogen receptor-related receptor (ERR) agonist with high affinity for ERRα, ERRβ, and ERRγ, exhibiting EC50 values of 98, 230, and 430 nM, respectively. SLU-PP-332 enhances mitochondrial function and cellular respiration, increases type IIa oxidized skeletal muscle fibers, and enhances exercise tolerance in skeletal muscle cell lines. It has potential applications in the study of metabolic diseases, improvement of muscle function, and amelioration of metabolic disorders and aging.

SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-selective prodrug of 17β-estradiol, which has neuroprotective effects, improves cognitive dysfunction, and can be used to study brain damage.

Acolbifene (SCH 57068) is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

Estradiol 3-sulfamate (BLE 00084) is an orally active and highly potent steroidal estrone sulfatase (ES) inhibitor.Estradiol 3-sulfamate has a K(i) value of 73 nM for ES in human placental microsomes and can be used in the study of breast cancer.

Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.

Camizestrant (Estrogen receptor antagonist 2) is an antagonist of the estrogen receptor and can be used in studies about ER+ HER2-advanced breast cancer[1].

Camizestrant TFA (AZD-9833 TFA) is a potent and orally active antagonist of estrogen receptor (ER).

Pipendoxifene hydrochloride is a selective modulator of estrogen receptor.

(Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.