Estrogen/progestogen Receptor

Tamoxifen (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

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.

Fulvestrant-d3 is a isotope labeled compound of Fulvestrant.Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist and GPR30 agonist that inhibits cell proliferation and induces apoptosis and autophagy.

(E Z)-4-Hydroxytamoxifen (Afimoxifene) is a novel estrogen inhibitor, commonly used in research for various estrogen-dependent conditions, including cyclic mastalgia and gynecomastia.

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.

Kaempferol (Robigenin) is a natural flavonoid and an inverse agonist of ERRα and ERRγ. Kaempferol has a wide range of antitumor, anti-inflammatory, antioxidant, antibacterial and antiviral activities.

XR 5944 is an antitumor compound that targets DNA, is a topoisomerase inhibitor, inhibits ER activity, and can be used to study colon and lung cancer.

Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.

Indazole-Cl is a selective ERß agonist and a selective estrogen receptor modifier (SERM).

Liquiritigenin (4',7-Dihydroxyflavanone), a flavonoid aglycone from licorice, is a highly selective estrogen receptor β (ERβ) agonist.

Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Bazedoxifene acetate (WAY-TES 424) is a novel selective estrogen receptor modulator (SERM).

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

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.

Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader .

Palazestrant (OP-1250) is an orally available and highly potent estrogen receptor antagonist and selective ER degrader with antitumor activity.Palazestrant inhibits 17b-estradiol (E2), inhibits MCF7 and CAMA-1 cell proliferation, and can be used in breast cancer research.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Progesterone (Pregn-4-ene-3,20-dione) is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production.

Erteberel (LY500307) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Propyl pyrazole triol (PPT) is a selective agonist of estrogen receptor alpha (ERα), exhibiting a relative binding affinity of 49% for ERα, which is approximately 410 times higher than its affinity for estrogen receptor beta (ERβ: 0.12%).

Amcenestrant (SAR439859) is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).

Natamycin (Pimaricin) is a Polyene Antimicrobial.

kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activation.

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

XCT790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα).

Hinokitiol (4-Isopropyltropolone) can inhibit ultraviolet B-induced apoptosis in keratinocytes and strongly suggest that the inhibitory mechanism is due to the antioxidant activity of metallothionein induced by the agent. Also, Hinokitiol modulates estrogen receptor signaling and inhibits proliferation of human breast cancer cells.

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

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).

Estradiol benzoate (Benzhormovarine) is the synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females.

Dienogest (STS 557) is an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive.

Medroxyprogesterone is used in the treatment of renal carcinoma. It is a synthetic progestational hormone used in veterinary practice as an estrus regulator.

Nestoron (Segesterone Acetate), a synthetic progestin, is a high-affinity agonist of the progesterone receptor (EC50: 10.3 nM).

H3B-6545 is a selective estrogen receptor covalent antagonist (SERCA) that is orally available. As a novel class of ERα antagonists, H3B-6545 is used in the study of metastatic breast cancers, such as estrogen receptor-positive (ER), human epidermal growth factor receptor 2-negative (HER2-) breast cancer.

Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM).

Estriol (Oestriol) is a hydroxylated metabolite of ESTRADIOL or ESTRONE that has a hydroxyl group at C3, 16-alpha, and 17-beta position. Estriol is a major urinary estrogen. During PREGNANCY, a large amount of estriol is produced by the PLACENTA.

17α-Hydroxyprogesterone (17-OHP) is a physiological progestin that is produced during glucocorticoid and steroid hormone synthesis and is increased during the third trimester of pregnancy. Hydroxyprogesterone binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor-mediated gene expression.

Pregnanediol (5Beta-Pregnane-3Alpha,20alpha-Diol) is an inactive metabolite of PROGESTERONE by reduction at C5, C3, and C20 position. Pregnanediol(5Beta-Pregnane-3Alpha,20alpha-Diol) has two hydroxyl groups, at 3-alpha and 20-alpha. It is detectable in URINE after OVULATION and is found in great quantities in the pregnancy urine.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

Clomiphene citrate (NSC 35770) is a selective estrogen receptor modulator.

AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity.

H3B-5942 belongs to a class of ERα antagonists referred to as selective estrogen receptor covalent antagonists (SERCA).

Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.

Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. Thymopentin (TP5) is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.