Estrogen/progestogen Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

Estrogen/progestogen Receptor Products

New Estrogen/progestogen Receptor Products
Catalog No. Information Product Use Citations Product Validations
S8372

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S5910New

Alpha-Estradiol

Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.

S9207

Gypenoside XVII

Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.

S4440New

2-Phenylacetamide

2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.

S5364

DY131

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).

S9609New

Amcenestrant (SAR439859)

Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.

S6651

G15 (GRB-G15)

G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.

S8746

H3B-5942

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.

S8686

PHTPP

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

S8958

AZD9833

AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.

S0851

G-1

G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.

S3449New

GSK5182

GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.

S0358

GSK4716

GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.

S4097

Dydrogesterone

Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.

S0407

XCT790

XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.

S5464

Psoralidin

Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.

S5469

Bavachin

Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.

S0503

Estrogen receptor modulator 1

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity.

S9520

Lasofoxifene Tartrate

Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM.

S6927New

Dihydroresveratrol

Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.

S5738New

Megestrol

Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.

S8956New

(Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.

S2301

Genistin (Genistoside)

Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.

S9122

Tectorigenin

Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.

S5785New

Norethindrone acetate

Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.

S4418New

Phenol Red sodium salt

Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells.

Catalog No. Information Product Use Citations Product Validations
S8372

AZD9496

AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.

S5910New

Alpha-Estradiol

Alpha-Estradiol (α-Estradiol, 17 alpha-Estradiol, Alfatradiol, Epiestradiol, Epiestrol, Alora, 17 α-E2), a natural, non-feminizing stereoisomer, a hormonally almost inactive isomer of physiological 17 beta-estradiol (17 β-E2), is a weak inhibitor of estrogen.

Catalog No. Information Product Use Citations Product Validations
S9207

Gypenoside XVII

Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.

S4440New

2-Phenylacetamide

2-Phenylacetamide, the main compound isolated from the seeds of Lepidium apetalum Willd (LA) with estrogenic activities, increases the expression of Estrogen receptorα (ERα), ERβ and GPR30 in the uterus and MCF-7 cells.

S5364

DY131

DY131 is a potent and selective ERRβ/γ activator. It has no effect on the structurally related receptors ERRalpha or the estrogen receptors alpha and beta (ERalpha/beta).

Catalog No. Information Product Use Citations Product Validations
S9609New

Amcenestrant (SAR439859)

Amcenestrant (SAR439859, compound 43d) is an orally available and nonsteroidal selective estrogen receptor degrader (SERD) with potential antineoplastic activity. SAR439859 is a potent estrogen receptor (ER) antagonist with EC50 of 0.2 nM for ERα degradation.

S6651

G15 (GRB-G15)

G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.

S8746

H3B-5942

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.

S8686

PHTPP

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

S8958

AZD9833

AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.

S0851

G-1

G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.

Catalog No. Information Product Use Citations Product Validations
S3449New

GSK5182

GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.

S0358

GSK4716

GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.

S4097

Dydrogesterone

Dydrogesterone (NSC 92336) is an orally active progestogen which acts directly on the uterus, producing a complete secretory endometrium in an estrogen-primed uterus.

S0407

XCT790

XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.

S5464

Psoralidin

Psoralidin, a naturally occurring coumestan isolated from the fractions of organic solvents such as ethylacetate, hexane, or n-butanol of the seed extract of Psoralea corylifolia L., has a variety of biological activities such as anticancer, antioxidant, antibacterial, antidepressant, anti-inflammatory activities, and regulation of insulin signaling. It is an agonist for both estrogen receptor (ER)α and ERβ with binding affinities (IC50s) of 1.03 and 24.6 μM, respectively.

S5469

Bavachin

Bavachin (Corylifolin) is a phytoestrogen purified from natural herbal plants such as Psoralea corylifolia. It acts as a weak phytoestrogen by binding and activating the ER.

Catalog No. Information Product Use Citations Product Validations
S0503

Estrogen receptor modulator 1

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM) with pIC50 of 0.46. Estrogen receptor modulator 1 exhibits potential anti-tumor activity.

S9520

Lasofoxifene Tartrate

Lasofoxifene Tartrate is a third-generation, non-steroidal selective estrogen receptor modulator (SERM) which binds with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM.

S6927New

Dihydroresveratrol

Dihydroresveratrol is a natural product possessing significant biological activities. Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator.

S5738New

Megestrol

Megestrol, a synthetic progestin, is approved for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis. Megestrol acetate (Megace) is one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer.

S8956New

(Z)-4-Hydroxytamoxifen

(Z)-4-Hydroxytamoxifen ((Z)-4-OHT, trans-4-Hydroxytamoxifen, 4-Monohydroxytamoxifen) is a selective modulator of estrogen receptor (SERM) with IC50 of 3.3 nM for the [3H]oestradiol binding to oestrogen receptor.

S2301

Genistin (Genistoside)

Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.

S9122

Tectorigenin

Tectorigenin (TEC) is an isoflavone isolated from various medicinal plants, such as Pueraria thunbergiana Benth, Belamcanda chinensis, and Iris unguicularis. It has been reported to exert pharmacological actions, including antitumor and antibacterial effects, free radical neutralization, and selective estrogen receptor modulation.

Catalog No. Information Product Use Citations Product Validations
S5785New

Norethindrone acetate

Norethindrone acetate (19-Norethindrone acetate, NA) is a common synthetic hormone used in oral contraceptives. Norethindrone acetate is a well-tolerated, effective option to manage pain and bleeding for all stages of endometriosis.

S4418New

Phenol Red sodium salt

Phenol Red sodium salt (Phenolsulfonephthalein sodium salt) is used ubiquitously as a pH indicator in tissue culture media ranging from 6.8 (yellow) to 8.2 (red). Phenol red binds to the estrogen receptor of MCF-7 human breast cancer cells.