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.

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.

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

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

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

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

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

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

Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader with IC50s of 48 for ERα and 870 nM for ERβ, respectively.

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

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.

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.

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.

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.

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.

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.

PHTPP is a selective ERβ antagonist.

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

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.

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.

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).

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

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.

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).

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.

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

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

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.

Diethylstilbestrol (DES) is used in the treatment of menopausal and postmenopausal disorders.

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

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%).

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

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

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

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

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

Ulipristal acetate (CDB-2914) is an orally bioavailable selective progesterone receptor modulator with anti-progesterone activity. It binds to the progesterone receptor (PR), inhibiting PR-mediated gene expression and interfering with progesterone activity in the reproductive system, potentially suppressing the growth of uterine leiomyomatosis. Additionally, ulipristal can be used as emergency contraception by inhibiting or delaying ovulation and affecting endometrial tissue.

Levonorgestrel (D-Norgestrel) is a Progestin and Progestin-containing Intrauterine Device. The physiologic effect of levonorgestrel is by means of Inhibit Ovum Fertilization.

Norgestrel (WY-3707) is a synthetic progestin commonly used alone or in combination with an estrogen for contraception. Norgestrel suppresses the secretion of luteinizing and follicle-stimulating hormones (LH and FSH), thickens cervical mucus, and slows the transit of ova through the fallopian tubes.

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.

WAY-200070 is a specific agonist of estrogen receptor β (ERRβ, IC50: 2.3 nM).

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.

Allura Red AC (CI 16035) is a very important food azo dye used in the food, pharmaceutical, paper, cosmetic and textile industries.Allura Red AC promotes susceptibility to experimental colitis via mouse intestinal serotonin.