AMG-34 is a GCN2-targeting agent with IC50 values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, PERK, HRland PKR, respectively.

VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes.

8(9)-EET is a major cytochrome P450 (CYP450) metabolite in the renal cortex[1][2]. It activates PPARα in HEK293 cells when used at a concentration of 1 μM but inhibits NF-κB activity induced by IL-1β in a PPARα-dependent and -independent fashion. It is also a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM .

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.

Deutaleglitazar (Aleglitazar-d2) is a agonist of dual peroxisome proliferatory activating receptor (PPARα and PPARγ).

IA107 is a potent, selective, and allosteric IRE1α RNase (IC50 = 16 nM (non phosphorylated), IC50 = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity.

Y502-2304 is a c-Myc G-quadruplex stabilizer. Y502-2304 exhibits potent antiproliferative activity in multiple myeloma (MM) cells. Y502–2304 downregulates c-Myc mRNA and protein expression. Y502-2304 induces apoptosis in MM cells, characterizes by elevated γH2AX levels, increases reactive oxygen species (ROS) generation, and mitochondrial dysfunction. Y502-2304 significantly inhibits tumor growth in a xenograft MM model. Y502-2304 can be used for the study of multiple myeloma.

SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133+/CD44+ cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers.

NVS2.1 is a potent, orally active and brain-penetrant readthrough promoter. NVS2.1 triggers the degradation of eRF1 by activating the ribosome-related quality control pathways (involving GCN1, RNF14, and RNF25), thereby facilitating the reading through of premature termination codons. NVS2.1 can be used for the research of genetic diseases caused by nonsense mutations.

CF-Carvacrol is an orally active lipid-lowering agent synthesized by merging the pharmacophores of Carvacrol and Clofibric acid. CF-Carvacrol has a good affinity for PPAR-α. CF-Carvacrol has significant hypolipidemic activity and may exert antioxidant and anti-inflammatory activity by activating the Nrf2/HO-1 signaling pathway to reduce liver injury. CF-Carvacrol can be used for the study of CF-induced liver damage.

GW9820 is PPARα and PPARγ activator (EC50s: 0.37 μM for PPARα; 0.288 μM for PPARγ). GW9820 increases CLA-1. GW9820 can be used in the research of atherosclerosis.

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.

ZLN005 (hydrochloride) is a peroxisome proliferator-activated receptor-g coactivator-1a (PGC-1α) activator. ZLN005 (hydrochloride) can stimulate the expression of PGC-1α and downstream genes in skeletal muscle cells, improve glucose utilization and fatty acid oxidation. ZLN005 (hydrochloride) can increase the transcription of PGC-1α and downstream genes in skeletal muscle of diabetic db/db mice, increase fat oxidation and improve glucose tolerance, pyruvate tolerance and insulin sensitivity.

AR ligand-44 TFA is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051.

AR ligand-44 is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051.

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.

Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research[1][2].

Cholic acid-Glu is a derivative of Cholic acid. The abundance of Cholic acid-Glu is increased in Crohn’s disease. Cholic acid-Glu increases PXR activation and significantly increases the expression of the downstream PXR target gene Cyp3a11 in small intestinal organoid tissue.

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.

EIDD-036, is the blood-brain barrier penetrant C-20 oxime of Progesterone, that binds progesterone receptor (PR) with an IC50 of 171 nM. EIDD-036 is the active metabolite of EIDD-1723. EIDD-036 exhibits promising challenges for rapid administration in acute trauma. EIDD-036 can be used for the study of traumatic brain injury (TBI).

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.

ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research.

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.

12-Nitrolinoleate (12-Nitro-9-cis,12-cis-octadecadienoic acid) is an activator for peroxisome proliferator-activated receptor γ (PPARγ). 12-Nitrolinoleate is a nitrated form of linoleic acid. 12-Nitrolinoleate can be formed upon exposure to acidified nitrate and found in human red blood cells and plasma. 12-Nitrolinoleate can activate PPARγ-dependent gene expression in MCF-7 cells expressing PPARγ with an EC50 = 0.045 μM. 12-Nitrolinoleate is able to inhibit LPS-induced NF-κB transcription in RAW 264.7 cells. 12-Nitrolinoleate can inhibit IL-6, TNF-α and CCL2 induced by LPS.

LCI765 is an orally active and selective PPARδ agonist, with an EC50 of 0.07 nM. LCI765 can be used for the research of diseases related to energy homeostasis such as metabolic syndrome.

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

KRP-105 is a potent, highly selective, and orally effective PPAR alpha (EC50 = 8 nM) agonist. KRP-105 can significantly reduce serum triglyceride, total cholesterol, and non high density lipoprotein cholesterol levels. KRP-105 can be used for research on metabolic diseases such as dyslipidemia.

CH4933468 is a thiohydantoin derivative, shows androgen receptor (AR) pure antagonist activity in vitro. CH4933468 inhibits AR-mediated transactivation and proliferation of LNCaP and LNCaP-BC2 cells. CH4933468 can be used for castration-resistant prostate cancer (CRPC) research.

(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.