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.

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.

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.

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 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 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.

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.

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

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).

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

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

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

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.

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.

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.

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.

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).

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) .

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 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 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).

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

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).

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.

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.

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

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.

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

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

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.