Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.

ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A.

DC360 is a synthetic retinoid analogue of all-trans retinoic acid (ATRA) which induces RARβ expression. DC360 can be utilized in characterization of retinoid signalling pathways.

BMS-185354 is a selective RARγ activator with an EC50 value of 28 nM. BMS-185354 is promising for research of cancers.

Onapristone is a progesterone receptor antagonist, with Kds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. Onapristone has antitumor activity.

11α-Hydroxytestosterone is a deriviative of Hydrocortisone, with the relative binding affinity to progesterone receptor of 9% (comparing to R5020119384) 100%). 11α-Hydroxytestosterone inhibits the growth and differentiation of human decidual cells in culture.

SP-C01 is an orally active soluble epoxide hydrolase (sEH) inhibitor and partial PPARγ agonist. SP-C01 can inhibit Ser273 phosphorylation.

SKLB102 shows a high affinity with PPARγ. SKLB102 has potent ability to reduce fat deposition and protect liver against non-alcoholic fatty liver disease (NAFLD) through regulating adipocytokine expression and preventing insulin resistance.

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.