PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer.

SR 16234 (TAS-108) is a selective estrogen receptor modulator. SR 16234 is promising for research of pain symptoms associated with endometriosis.

(S)-STO021 is a highly selective, orally effective ERβ agonist. (S)-STO021 has a dual activity of inhibiting osteoclast activity and promoting osteoblast activity. (S)-STO021 can be used for research on osteoporosis.

F0840-0093 is a highly selective estrogen receptor α (ERα) degrader. F0840-0093 exhibits potent antiproliferative activity against T47D cells with an IC50 value of 4.65 μM. F0840-0093 is promising for research of estrogen receptor-positive (ER+) breast cancer.

MK-8389 is an orally active LMW allosteric FSH receptor agonist. MK-8389 affects thyroid function.

ER ligand-11 is the ligand for ERα and can be used for synthesis of PROTACs, such as PROTAC ERα Degrader-12.

ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer.

CIMBA hydrochloride is a selective G protein-coupled estrogen receptor (GPER) antagonist. CIMBA hydrochloride is used in the research of cholesterol gallstones in women.

14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research.

AZD9496-O-C3-O-C3-O-C-acid is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for ERα and a PROTAC linker, which recruits E3 ligases. AZD9496-O-C3-O-C3-O-C-acid can be used for synthesis of PROTAC AZ'6421.

NKS-01 is a selective estrogen receptor modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer.

NDC 1308 is an estradiol analogue. NDC 1308 can bind estrogen receptor beta and inhibit cancer cell proliferation by blocking chromosome replication. NDC 1308 can be used for the research of cancer, such as breast cancer.

HMR-3339 is a new selective estrogen receptor modulator. HMR-3339 reduces total cholesterol, low-density lipoprotein cholesterol, and homocysteine. HMR-3339 corrects bone alterations induced by ovariectomy.

RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research.

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant in combination with a HER2 inhibitor, works on ER+/HER2+ cancer.

WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of ERβ.

WAY-166818 (WAY-818) is a synthetic nonsteroidal estrogen that is a selective agonist of ERβ.

PBPE hydrochloride is a derivative of tamoxifen.

Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer.

LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes.

Hexolame is an estrogen receptors agonist with dual anticoagulant and estrogenic properties. Hexolame binds to estrogen receptors to induce anticoagulant effects by modulating clotting factors or platelet activity. Hexolame is promising for research of prostatic cancer and prevention of thrombosis.

GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.

Estrone acetate (Hogival) is an estrogen derivative and an estrogen receptor (ER) activator. It promotes mammary gland development, stimulates pituitary prolactin secretion, and induces the proliferation and activation of lactotrophs (e.g., by reducing prolactin storage granule size while increasing rough endoplasmic reticulum and Golgi apparatus volume density). Estrone acetate holds potential for endocrine research, particularly in studying estrogen's effects on pituitary function, prolactin regulation, and mammary tumor models.

2,3,4-Trihydroxybenzophenone is a hydroxylated benzophenone UV filter with estrogenic activity. 2,3,4-Trihydroxybenzophenone is a quorum sensing inhibitor and an EC 1.14.18.1 (tyrosinase) inhibitor. 2,3,4-Trihydroxybenzophenone is also a human urinary metabolite, a rat metabolite and a drug metabolite.

(E/Z)-Panomifene (hydrochloride) is an orally active tamoxifen (TMX), thereby suppressing tumor growth both in vitro and in vivo.

(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity.

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).

ARV471 is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

(E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.

SLU-PP-332 is a potent, selective pan ERRα/β/γ agonist with EC50 of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, in full-length ERR cell-based cotransfection/reporter assays.