FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the treatment of fatty liver disease.

Enzalutamide D3 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

(rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (rac)-PF-998425 has the potential for the research of the androgenetic alopecia.

Imlunestrant (LY3484356) is an orally active selective estrogen receptor (ER) degrader (SERD). Imlunestrant (LY3484356) could be used in the study for ER+, HER2-advanced breast cancer.

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.

eIF4A3-IN-6 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-6 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1).

eIF4A3-IN-5 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-5 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1).

eIF4A3-IN-7 is a potent inhibitor of eIF4A3. eIF4A3-IN-7 has the potential for researching cancer and other dysproliferative diseases (extracted from patent WO2019161345A1, Compound 8).

eIF4E-IN-3 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-3 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 485).

eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y).

eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-2 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 1188).

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).

Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).

Naphthofluorescein inhibits the interaction between HIF-1 and Mint3. Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging.

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.

Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the treatment of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1).

Vutiglabridin is a synthetic structural analog of glabridin for the treatment of obesity.

Rivoglitazone is a thiazolidinedione-derivative PPARγ agonist for the treatment of type 2 diabetes mellitus.

Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.

KRP-297 is a PPARα and PPARγ agonist potentially for the treatment of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.

Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.

Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b).

10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM.

Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1.

BAY 1003803 is a glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis.

SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).

Indolokine A4, a catabolite of indole-3-pyruvate (I3P), is a potent AhR agonist.

Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist.

HG122 promotes androgen receptor (AR) degradation through the proteasome pathway inhibiting the castration-resistant prostate cancer.

RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC50s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity.

RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity.

Cholesterol-13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.

RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research.

Estradiol enanthate is a shorter-acting estrogen. The combination of Estradiol enanthate and dihydroxyprogesterone acetophenide can be used as a monthly injectable contraceptive.

AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism.

Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic.

ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis.

Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels.

Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4+ T cells and CD11b+ macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM.

c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes.

DK3 is a potent and selective estrogen-related receptor alpha (ERRα) agonist.

DK1 is a potent modulator of estrogen related receptor. DK1 has an ability in reducing blood glucose, and impacts the activity of ERRα receptor. DK1 has the potential for the research of diabetes.

Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165).

Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166).

Ethynyl Estradiol-13C2 (17α-Ethynylestradiol-13C2) is the 13C-labeled Ethynyl Estradiol.

Estriol-d3-1 (Oestriol-d3-1) is the deuterium labeled Estriol.

Estrone-d4 (E1-d4) is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.

Estradiol-13C2 (β-Estradiol-13C2) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

Estrone-13C2 (E1-13C2) is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.

Estradiol-13C6 (β-Estradiol-13C6) is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

2-Hydroxyestrone 3-methyl ether-13C is the 13C-labeled 2-Hydroxyestrone 3-methyl ether. 2-Hydroxyestrone 3-methyl is an estrogen metabolite.

ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the treatment of breast cancer.

ERRγ agonist-1 is a potent ERRγ agonist. ERRγ agonist-1 increases transcriptional activities of ERRγ. ERRγ agonist-1 has the potential for the research of neuropsychological disorders.

KUSC-5001 is a potent HIF-1 inhibitor with an IC50 of 18 μM. Hypoxia-inducible factor 1 (HIF-1) plays a pivotal role in tumor survival and malignancy.

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.

HIF-PHD-IN-2 (compound 25) is a potent PHD inhibitor with IC50s of <100 nM for PHD1, PHD2 and PHD3, respectively.

HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.

SR2595 is an inverse agonist of PPARγ with an IC50 of 30 nM.

AZD9574 is a CNS-penetrant, PARP1-selective inhibitor with IC50 of <0.005 μM. AZD9574 demonstrates >10,000-fold selectivity for PARP1 over PARP2 and shows excellent preclinical PK acrossseveral species, with low clearance and high oral bioavailability, and demonstrated in vivo efficacy in a BRCA2−/− DLD-1 mouse xenograft model.

PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis.

Progesterone-13C2 (Pregn-4-ene-3,20-dione-13C2) is the 13C-labeled Progesterone. Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.

BMS641 (BMS-209641) is a selective RARβ agonist. BMS641 has a higher affinity for RARβ (Kd, 2.5 nM) that is 100 times higher than that for RARα (Kd, 225 nM) or RARγ (Kd, 223 nM).

ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.

RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2).

RORγt modulator 4 is a RORγt modulator. RORγt modulator 4 has an activity to modulate IL-17A production in cells derived from mouse spleen (WO2018030550A1; compound 146).

RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .

RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .

Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43).

NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.

BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis.

Chenodeoxycholic acid-d5 (CDCA-d5) is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

Chenodeoxycholic acid-13C (CDCA-13C) is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

Hydrocortisone-d3 (Cortisol-d3) is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex.

Cortodoxone-d5 (11-Deoxycortisol-d5) is the deuterium labeled Cortodoxone.

Cortodoxone-d2 (11-Deoxycortisol-d2) is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone).

Glucocorticoids receptor agonist 3 is a potent agonist of glucocorticoids receptor. Glucocorticoids receptor agonist 3 is useful to research diseases, such as obesity, diabetes, and inflammation (extracted from patent WO2000066522A1, compound 345).

GSK-2324 (GSK2324) is a potent, selective, full FXR agonist with EC50 of 120 nM in FRET assay.

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

3JC48-3 is a potent, cellularly active and stable c-Myc inhibitor, inhibits c-Myc-max dimerization with IC50 of 34 uM, 5 times more potent than 10074-G5, exhibits an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers.3JC48-3 inhibited the proliferation of c-Myc-over-expressing HL60 and Daudi cells with single-digit micromolar IC50 values by causing growth arrest at the G0 /G1 phase.3JC48-3 inhibited c-Myc-Max dimerization in cells validated by CoIP.3JC48-3 decreased prostate cancer cells' growth and viability in a dose-dependent fashion in vitro, upregulated PrKD1 expression and phosphorylation of known PrKD1 substrates: the threonine 120 (Thr-120) residue in beta-catenin and the serine 216 (Ser-216) in Cell Division Cycle 25 (CDC25C).3JC48-3 (1 g/kg, i.p.) decreased the rate of tumor growth in mice with patient-derived prostate cancer xenografts (PDX), without dose-limiting toxicity.

A novel potent IRE1α-selective kinase inhibitor that inhibits both the kinase and RNase activities of IRE1α with IC50 of 20 nM and 200 nM, respectively; binds to pIRE1α and inhibits XBP 1 splicing; only weakly inhibits Ron (IC50= 4.4 uM) and FGFR1 V561M (IC50=17 uM) in a panel of 284 kinases.

A potent, selective, orally active LXR agonist that recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM; acts as a full agonist on hLXRα and hLXRβ in cell-based reporter gene assays with EC50 of 190 and 30 nM, respectively; increases expression of ABCA1 in the small intestine and peripheral macrophages in C57BL/6 mice at 10 mg/kg.

A synthetic vitamin D3 analog that usually prescribed by a general practitioner or dermatologist for the treatment of psoriasis, chronic chapped lips and other severe dry skin conditions.

A-9758 (A9758) is a selective, small molecule inverse agonist of retinoid-related orphan receptor gamma t (hRORγt IC50=38 nM).A-9758 also inhibits mouse RORγ transactivation with similar activity (20 nM) and is equally active on dog and rat RORγ (25 and 64 nM, repectively).A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM in human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively.A-9758 exhibits robust potency against IL-17A release both in vitro and in vivo, significantly attenuates IL-23 driven psoriasiform dermatitis.A-9758 exhibits efficacy in an ex vivo human whole blood assay, is efficacious in human IL-17 related diseases.

Artepillin C (CREB-CRTC2 inhibitor APC) is an inhibitor of CREB/CRTC2 interaction (IC50=24.5 uM), dissociates the CREB/CRTC2 complex, directly binds to CREB with Kd of 3.2 uM.CREB-CRTC2 inhibitor APC inhibits CRTC2 interacting with CREB-ZIP and reduces acetyltransferase activity of CBP by binding with CREB protein directly.Artepillin C attenuated gluconeogenesis in primary hepatocytes, reduced glucose output from primary hepatocytes induced by glucagon, remarkably decreased the mRNA accumulation of G6pc, Pck1, and Pgc-1α induced by glucagon in primary hepatocytes.|Artepillin C could ameliorate hyperlipidemia in obese mice.

BC-N102 is a first-in-class novel small molecule inhibitor for targeting oncogenic and hormonal signaling in ER-positive breast cancer.BC-N102 exhibits anticancer activity against breast cancer cell lines via interfering with cell cycle regulatory proteins and hormonal receptors signaling in vitro (IC50=0.04-10 uM), no significant activities against a normal breast cell line.BC-N102 exhibits potent antitumor activity at tolerated doses in an ER+ human xenograft breast cancer model.BC-N102 induces arrest of the cell cycle at G0/G1 phase, downregulates the expression of CDK2 and CDK4 independent of the ER in breast cancer cell lines.

BMS-986313 is a potent, selective, orally active RORγt inverse agonist with EC50 of 3.6 nM in GAL-4 reporter assay in Jurkat cell line, and 50 nM in IL-17 human whole blood assay.BMS-986313 demonstrated robust efficacy in preclinical models of psoriasis (the IMQ-induced skin lesion model and the IL-23-induced acanthosis model).

Cl-OCH3 is an antagonist of nuclear receptor NR4A1, decreases PD-L1 protein expression in MDA-MB-231 and 4T1 cells with EC50 of 4.4 and 4.1 uM, respectively; Cl-OCH3 decreased expression of PD-L1 mRNA, promoter-dependent luciferase activity, and protein. In in vivo studies using a syngeneic mouse model bearing orthotopically injected 4T1 cells, Cl-OCH3 decreased tumor growth and weight and inhibited lung metastasis. Cl-OCH3 also decreased expression of CD3+/CD4+/CD25+/FoxP3+ regulatory T cells and increased the Teff/Treg ratio.

Cobalt protoporphyrin IX (CoPPIX) is a potent and effective inducer of HO-1 (heme oxygenase-1) activity, up-regulates HO-1 via Bach1 and Nrf2 in human liver cells.CoPPIX did not influence hepatic Bach1 or Nrf2 mRNA levels, but markedly reduced Bach1 protein levels by increasing degradation of Bach1 protein, and increased Nrf2 by decreasing degradation of Nrf2 protein.CoPPIX significantly upregulated HO-1 protein in mucosal and submucosal cells.CoPPIX is a direct Bach1 inhibitor.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

DC-TEADin1072 is a novel TEAD1/3 covalent inhibitor with biochemical IC50 values of 0.61 and 0.58 uM against TEAD1 and TEAD3, respectively.TEADin1072 selectively inhibited TEAD1 and TEAD3 palmitoylation while sparing TEAD2 and TEAD4.TEADin1072 demonstrated selective engagement with Cys371 of TEAD3 and Cys359 of TEAD1.

DN200434 (DN-200434) is a highly potent (functional IC50=6 nM, binding IC50=40 nM), selective, biocompatible and orally available ERRγ inverse agonist.DN200434 binds to key ERRγ binding pocket residues through four-way interactions.DN200434 effectively upregulated iodide-handling genes and restored radioiodine avidity in ATC tumor lesions.DN200434 enhanced ATC tumor radioiodine therapy susceptibility, markedly inhibiting tumor growth.DN200434 shows higher potency than GSK5182.

EGPI-1 is a potent small molecule that inhibits the translation initiation factors eIF4E/eIF4G interaction.EGPI-1 has potent antiproliferative and proapoptotic activity in multiple myeloma cells, Jurkat cells, and A549 lung cancer cell lines, inhibts A549 proliferation with IC50 of 2.61 uM, which is better than that of 4EGI-1 (IC50=58.6 uM), inhibits cancer cell growth by inhibiting eIF4E phosphorylation and inhibiting PI3K/Akt/mTOR signal pathway.EGPI-1 induces autophagy, apoptosis, G0/G1 cell cycle arrest and ROS generation in A549 cells, disrupts the mitochondrial membrane potential (∆ψ m).EGPI-1 demonstrated in vivo anti-tumor activities in A549-xenografted athymic mice (25 mg/kg/day, 50 mg/kg/day, i.p.).

Exicorilant (CORT125281, CORT-125281) is a potent, selective glucocorticoid receptor (GR) antagonist, exhibits no cross-reactivity for the PR and AR receptors.

F0909-0360 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=0.2 uM).F0909-0360 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F0909-0360 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 4.06 uM.

F1021-0686 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=1.55 uM).F1021-0686 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F1021-0686 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 5.27 uM.

GSK-2945 is a potent and selective small molecule Rev-Erbα agonist with EC50 of 50 nM, displays >1,000-fold selectivity over LXRα; inhibits LPS induction of IL-6 production and to upregulate expression of ABCA1 in human THP-1 cells; demonstrates in vivo bioavailability and orally active.

HIF inhibitor 208 is a small molecule inhibitor of HIF pathway with IC50 of 0.5 nM.

HPPE is a specific nonelectrophilic and physiological Bach1 inhibitor via heme-binding sites of Bach1 protein, derepresses Bach1-mediated repression.HPPE induces up-regulation of Hmox1 mRNA is mediated by Bach1 inhibition in vivo.

JNJ-pan-AR is a highly potent, selective antagonist of androgen receptor (AR) wild-type and F877L mutant for the treatment of the F877L mutant and wild-type CRPC.

KI-696 (KI696) is a highly potent, selective inhibitor of KEAP1-NRF2 interaction, exhibits very high affinity for the KEAP1 Kelch domain with ITC Kd of 1.3 nM.KI-696 displays high selectivity against a panel of 49 in vitro functional assays for targets, with the exception of the OATP1B1 (IC50=2.5 µM), the bile salt export pump BSEP (IC50=4.0 µM), and PDE3A (IC50=10 uM).KI-696 increases NRF2 nuclear translocation in normal human bronchial epithelial cells, up-regulates NRF2-dependent gene expression NQO1 and GCLM, and increases NQO1 activity in an NRF2-dependent manner.KI-696 significantly reduces ozone-induced pulmonary inflammation, restores ozone-induced depletion of lung GSH levels in vivo.

KUSC-5037 (KUSC5037) is a novel effective HIF-1 inhibitor with IC50 of 1.2 uM against HIF-1 transcriptional activity.KUSC-5037 suppressed the HIF-1α (a regulatory subunit of HIF-1) mRNA, causing decreases in the gene expression of HIF-1 target genes such as carbonic anhydrase 9 (CA9) and vascular endothelial growth factor (VEGF) genes.KUSC-5037 directly targets ATP5B protein, a catalytic β subunit of mitochondrial FoF1-ATP synthase.

KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

LEO 134310 (LP 0155) is a non-steroidal, potent and selective glucocorticoid receptor (GR) agonist (EC50=2 nM, hPBMC)

MB 07811 (MB07811) is an orally bioavailable, liver-targeted prodrug of MB07344, which is a thyroid hormone receptor-beta agonist (TRβ) agonist, efficiently converted to MB07344 by liver microsomes in vivo; reduces cholesterol and both serum and hepatic triglycerides at doses devoid of effects on body weight, glycemia, and the THA.

MSU 38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth; MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream targets, including NQO1, GCLC, GCLM, AKR1C2, and UGT1A6. MSU38225 strikingly decreases the protein level of Nrf2, which can be blocked by the proteasome inhibitor MG132. Ubiquitination of Nrf2 is enhanced following treatment with MSU38225. By inhibiting production of antioxidants, MSU38225 increases the level of reactive oxygen species (ROS) when cells are stimulated with tert-butyl hydroperoxide (tBHP). MSU38225 also inhibits the growth of human lung cancer cells in both two-dimensional cell culture and soft agar.

MYCMI-7 is a small molecule MYC-binding compound (Kd=4 uM) that inhibits MYC-MAX interaction.MYCMI-7 efficiently and selectively inhibits MYC:MAX and MYCN:MAX interactions in cells, binds directly to recombinant MYC, and reduces MYC-driven transcription.MYCMI-7 induces degradation of MYC and MYCN proteins.MYCMI-7 potently induces growth arrest/apoptosis in tumor cells in a MYC/MYCN-dependent manner and downregulates the MYC pathway on a global level.MYCMI-7 downregulates MYC/MYCN, inhibits tumor growth, and prolongs survival through apoptosis in mouse tumor models of MYC-driven AML, breast cancer, and MYCN-amplified neuroblastoma.

NXT629 (NXT-629) is a potent, selective PPARα antagonist with IC50 of 77 nM (human PPARα), no effect against PPARδ and PPARγ (IC50>30 uM).NXT629 inhibited agonist-induced transcription of PPARα-regulated genes, demonstrating target engagement in chronic lymphocytic leukemia (CLL) cells.NXT629 induced apoptosis of CLL cells even in the presence of a protective microenvironment.NXT629 reduces the number of chronic leukemia cells undergoing cell division with IC50 of 9.6 uM.NXT629 reduces CLL tumor burden delays disease progression of CLL in CLL mouse model.

PKUMDL-YC-1205 is a specific small molecule that can specifically bind to the disordered bHLH-LZ domain of c-Myc (SPR kd=18 uM).PKUMDL-YC-1205 abrogates cell proliferation of HL-60 cells with IC50 of 40 uM, blocks the interaction between c-Myc370–409 and Max.

PPARγ pSer273-IN-10 is a specific, in vivo-active small molecule inhibitor of CDK5-mediated Ser273 phosphorylation of PPARγ without classical PPARγ agonism.PPARγ pSer273-IN-10 is a potent PPARγ binder and in vitro inhibitor of the CDK5-mediated phosphorylation of PPARγ Ser273 and displays negligible PPARγ agonism in a reporter gene assay. PPARγ pSer273-IN-10 demonstrated an improvement in insulin sensitivity in the ob/ob diabetic mouse model in 7 day treatment in vivo testing.

PRL295 is a small molecule Keap1-Nrf2 protein–protein interaction inhibitor.PRL295 binds to Keap1 in the cellular environment, disrupting its interaction with Nrf2, which leads to enhanced gene expression of the classical Nrf2 target NQO1 in cells and in vivo in the mouse liver.PRL-295 increases the thermostability of Keap1 in cell lysates and in live cells.PRL 295 decreased the levels of plasma alanine aminotransferase and aspartate aminotransferase upon acetaminophen-induced hepatic injury.

Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.

SR1555 is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells; SR1555 is devoid of LXR, FXR, and RORα activity, displaces [3H]T0901317 from the ligand binding domain (LBD) of RORγ with IC50 of 1 uM; represses the expression of RORγ while leading to increased expression of FGF21 and adipoQ in pre-adipocyctes, inhibits activation of hormone-sensitive lipase and increased fatty acid oxidation in obese diabetic mice.

TTC352 is a synthetic selective estrogen mimic acts as estrogen receptor (ER) partial agonist for the treatment of endocrine-resistant breast cancer.TTC 352 yields an H-bond with Glu353, allows Asp351-to-helix 12 (H12) interaction, sealing ERα's ligand-binding domain, recruiting E2-enriched coactivators, and triggering rapid ERα-induced unfolded protein response (UPR) and apoptosis.TTC-352 is a less potent full estrogen agonist compared to E2, allowing H12 to seal the LBD, which recruits many E2-enriched coactivators, and induces rapid ERα-mediated UPR and apoptosis.

VPC-13789 (VPC13789) is a potent, selective, orally available inhibitor of androgen receptor binding function-3 (BF3) site.VPC-13789 suppresses AR-mediated transcription, chromatin binding, and recruitment of coregulatory proteins.VPC-13789 selectively reduces the growth of both androgen-dependent and enzalutamide-resistant PCa cell lines.VPC-13789 demonstrated in vitro efficacy that reduced PSA production and tumor volume in animal models of CRPC with no observed toxicity.

VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.

WBC100 (WBC-100) is a novel potent, oral active that selectively degrades c-Myc protein over other proteins and potently kills c-Myc overexpressing cancer cell.selectively kills c-Myc overexpressing cancer cells Mia-paca2 (PDAC), H9 (T-cell lymphoma), andMOLM-13 (acute myeloid leukemia) with IC5 of 61, 17 and 16 nM, respectively.WBC100 targets the nuclear localization signal 1 (NLS1)-Basic-nuclear localization signal 2 (NLS2) region of c-Myc and induces c-Myc protein degradation through ubiquitin E3 ligase CHIP mediated 26S proteasome pathway, leading to apoptosis of cancer cells.WBC100 potently regresses multiple lethal c-Myc overexpressing tumors such as acute myeloid leukemia, pancreatic, and gastric cancers with good tolerability in multiple xenograft mouse models.

WO95E is a novel potent, synthetic ligand (partial agonist) of PPARγ, directly binds to PPARγ with IC50 of 11 nM; WO95E's binding affinity is approximately 70-fold lower than that of UHC1 (Journal of Biological Chemistry. 2014;289(38):26618–26629.). WO95E significantly inhibited the S273 phosphorylation of PPARγ in 3T3-L1 differentiated adipocytes, led to the upregulation of the mRNA levels of a number of the PPARγ phosphorylation-dependent genes, including adiponectin, cycp2f2, Ddx-17, Rarres2, and Selenbp1. Unlike SR1664 and UHC1, WO95E does not bind to the canonical PPARγ ligand-binding pocket (LBP) containing H3, H3-4 loop, H11 and H12, which full agonist Rosi binds, instead, WO95E binds to the ABP comprising H2′-H3, β-sheet, and the Ω loop. WO95E improved glucose tolerance and insulin sensitivity in DIO mice.

YQ-0629 is a specific HIF-2α inhibitor, binds to HIF-2α PAS-B domain with Kd of 57.5 uM.YQ-0629 could inhibit the expression of HIF-2α with or without the presence of PTX (3 nM) in MCF7 MS culture, does not bind to HIF-1α or affect the expression of HIF-1α.YQ-0629 suppresses self-renewal capacity and synergizes with PTX to reverse the chemoresistance of MCF7 MS.YQ-0629 inhibits growth of BCSCs derived from breast cancer patients and synergistically increases anti-BCSCs activity of PTX in vivo.

BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.

DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2 activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity.

Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a potent topical glucocorticoid. Hydrocortisone aceponate can be used for various dermatoses research.

S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ.

KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.

LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.

CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells.

Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity.

H-​Trp-​Glu-​OH is a selective, reversible and cell-permeable PPARγ with a Kd of ~8 µM. H-​Trp-​Glu-​OH might be developed as a possible lead compound in diabetes research.

PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm.

MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.

SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively.

Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities.

OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent.

PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing.

Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM.

11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).

(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4+ T cells into other lineages, including Th1 and regulatory T cells.

IZTZ-1, an imidazole-benzothiazole conjugate, is a c-MYC G4 ligand. IZTZ-1 is able to downregulate the c-MYC expression by stabilizing c-MYC G4. IZTZ-1 induces cell cycle arrest, apoptosis, thereby inhibiting cell proliferation in B16 cells. IZTZ-1 shows antitumor activity, and can be used for melanoma research.

Enclomiphene ((E)-Clomiphene) is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.

EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively.

EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively.

NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research.

2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation.

GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential.

Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.

Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms.

Adrenocorticotropic hormone (ACTH) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone regulates cortisol and androgen production.

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.

Lorundrostat is a aldosterone synthase inhibitor.

MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.

Enclomiphene ((E)-Clomiphene) dihydrochloride is a potent and orally active non-steroidal estrogen receptor antagonist, with antioestrogenic property. Enclomiphene dihydrochloride can be used for the research of ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.

FERb 033 is a selective and potent ERβ agonist (Ki=7.1 nM, EC50=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.

Taragarestrant (D-0502) is a potent, orally active estrogen receptor degrader. Taragarestrant has antiproliferative activity against estrogen receptor-positive breast cancer cell lines and has anticancer activity. Taragarestrant can be used for cancer research.

Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.

Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.

Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.

Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.

BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues.

Omesdafexor is a FXR agonist. Omesdafexor can be used in the research of liver disease or a metabolic inflammation-mediated disease.

Beclometasone dipropionate monohydrate, the prodrug of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate monohydrate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate monohydrate can be used for asthma .

Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research.

BE1218 is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM and 7 nM against LXRα and LXRβ, respectively.

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor.

ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression.

EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC).

DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent.

SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.

Norgestrienone, progestin or synthetic progestin, is a progestin receptor agonist. Norgestrienone is often used as a progestational compound in birth control pills and can be used in combination with ethinyl estradiol.

Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.

Oct4 inducer-1 (compound OAC-3) is a potent Oct4 activator. Oct4 inducer-1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. Oct4 inducer-1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.

DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM.

MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects.

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

Izumerogant is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM.

Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist.

RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castrated tolerant prostate cancer (mCRPC) cell line and can stably exist in vivo.

Dextrothyroxine (D-T4) sodium, a sodium salt of D-T4, is a laevorotatory isomer of thyroxine used for thyroid related studies.

Prepro-TRH-(160-169) is one of the connecting peptides of thyrotropin-releasing hormone prohormone (pro-TRH), potentiates TRH-induced thyrotropin (TSH) release.

2MD is an orally active vitamin D analog. 2MD stimulates periosteal bone formation and decreases trabecular bone resorption. Thus 2MD restores trabecular and cortical bone mass and strength. 2MD also regulates intraocular pressure (IOP)-relative genes and reduces IOP in non-human primates.

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.

IK930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expre

Faznolutamide is a potent, selective androgen receptor (AR) antagonist.

JJ-450 is a novel analogue of IMTPPE and direct and specific inhibitor of androgen receptor (AR) transcriptional activity, blocks AR recruitment to androgen-responsive elements and suppresses AR target gene expression.

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.

MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.

SC428 (SC-428) is a small molecule androgen receptor (AR) signaling inhibitor, directly binds to the AR N-terminal domain (NTD) and exhibits pan-AR inhibitory effect.

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).

UT-215 (UT215) is a small-molecule selective androgen receptor (AR) irreversible covalent antagonist, covalently and selectively bind to C406 and C327 in the AF-1 region of AR.

GDU-952 is a novel small molecule aryl hydrocarbon receptor (AhR) agonist, activates and induces nuclear translocation of AhR.

A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro.

D089 is a selective small molecule stabilizer of the MYC G4-quadruplex, not only inhibits MYC expression in myeloma cell lines, but also selectively induces G1 arrest in MYC-driven cancer cell lines containing the MYC-G4 sequence.

Isopomiferin is a prenylated isoflavonoid, collapses the tumor checkpoint module (TCM) and suppresses both MYCN and TEAD4 in MYCN-amplified NBL cells.

KSI-3716 is a small molecule c-MYC inhibitor that blocks c-MYC/MAX binding to target gene promoters, inhibits c-MYC mediated transcriptional activity at concentrations as low as 1 uM.