PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC50 value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro.

MHY 553 is a PPARα agonist that is effective when taken orally. MHY 553 helps alleviate liver fat accumulation by increasing fatty acid oxidation and reducing inflammation during the aging process. MHY 553 inhibits the accumulation of triglycerides induced by liver X receptor agonists in HepG2 cells. MHY 553 significantly suppresses the expression of inflammatory mRNA in aging rats.

E0924G is an orally active activator for PPARδ with EC50 of 2.82 μM. E0924G promotes the upregulation of osteoprotegerin (OPG) with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibites F-actin ring formation in RAW264.7 macrophages. E0924G regulates the bone density and bone loss in ovariectomized (OVX) and age-related osteoporosis models.

DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes.

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

Apo-12'-lycopenal is a Lycopene metabolite. Apo-12'-lycopenal promotes adipocyte differentiation and adiponectin secretion via PPAR-γ activation.

Amezalpat is the antagonist for PPARα with IC50 of 58 nM. Amezalpat exhibits antineoplastic activity.

AD-5075 is an orally active insulin sensitizer. AD-5075 mediates its antidiabetic activity by binding to PPARγ and thereby generating an active conformation of the receptor.

9(10)-Nitrooleate (9(10)-Nitrated oleic acid) is a nitrated derivative of Oleic acid. 9(1

(E)-CLX-0921 is the E-isomer of CLX-0921 with antiviral activity. 5-Oxo leukotriene B4 is promising for research of viral infections caused by human and animal enveloped RNA viruses.

(±)-CBCQ is an oxidative product of cannabichromene, with an EC50 of 14.7 μM for PPAR-γ.

IXA62 is an orally active and selective IRE1/XBP1s activator (EC50 = 0.31 μM) that reduces Aβ secretion. IXA62 enhances glucose-stimulated insulin secretion from rat insulinoma cells.

1ACTA is an IRE1α S-Nitrosylation inhibtor, maintaining the endoplasmic reticulum stress response under nitrosative stress.

Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD.

LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.

JPHM-2-167 (Compound 11) is a selective PHD (prolyl hydroxylase domain enzyme) inhibitor. JPHM-2-167 inhibits PHD2, PHD3 with IC50s of 0.253 μM and 3.95 μM, respectively. JPHM-2-167 can be used for chronic kidney disease .

DDO-3055 is an orally active PHD2 inhibitor that can be used in the research of anemia associated with chronic kidney disease.

3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research.

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.

NSC308848 is a potent apoptosis inducer in a Myc-dependent manner. NSC308848 inhibits Myc transactivation and interferes with the DNA-binding activity of Myc family proteins.