Teduglutide (ALX-0600) is a glucagon-like peptide-2 analog that increases intestinal absorption by promoting mucosal growth and reducing mucosal degradation, improving intestinal recovery. It is used in the study of short bowel syndrome (SBS). Teduglutide activates NR4a1/nur77 expression and FXR signaling, alleviating intestinal dysfunction in mice and improving lung injury, making it useful for studying metabolic and cardiovascular diseases.

Broussochalcone A is a natural antioxidant and xanthine oxidase inhibitor (IC₅₀ = 2.21 μM) that scavenges free radicals, inhibits iron-induced lipid peroxidation, and reduces nitric oxide synthesis in LPS-activated macrophages. Broussochalcone A induces apoptosis in human renal carcinoma cells by increasing ROS levels and activating the FOXO3 signaling pathway. Broussochalcone A is also a novel NR4A1 inhibitor that induces apoptosis in pancreatic cancer cells through NR4A1-dependent pathways.

Amodiaquine is a synthetic aminoquinoline, used to treat malaria.

Cytosporone B (Dothiorelone G) is a naturally occurring agonist of the nuclear orphan receptor Nur77/NR4A1 (EC₅₀=0.278 nM).

DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.

IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC₅₀ value of 3.9 nM.

Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.

TMPA is a nuclear receptor Nur77 and LKB1 interaction antagonist.

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

Nurr1 agonist 2 is a Nurr1 agonist with an EC₅₀ value of 0.07 μM. Nurr1 agonist 2 increases the mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand-binding domain (LBD) with a Kd of 0.14 μM. Nurr1 agonist 2 can be used to study parkinsonism.

Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

4-PQBH is a potent Nur77-binding agent with antitumour activity.4-PQBH inhibits xenograft tumours through Nur77-mediated endoplasmic stress and autophagy by broadly inducing cysteoaspartase-independent cytoplasmic vacuolisation and parapetaloid ptosis.4-PQBH is used in the study of hepatocellular carcinoma.4-PQBH is a potent Nur77-binding agent with antitumour activity.

C-DIM12 induced expression of Nurr1-regulated genes. C-DIM12 increased expression of transfected human Nurr1, induced Nurr1 protein expression in primary dopaminergic neurons and enhanced neuronal survival from exposure to 6-OHDA.

DIM-C-pPhOCH3 (C-DIM5) is a Nerve Growth Factor-Induced Bα (NGFI-Bα, Nur77) agonist

DIM-C-pPhCO2Me is an antagonist of nuclear receptor 4A1 (NR4A1).

Nurr1 agonist 8 is a low-affinity Nurr1 agonist that can be used to study neurological diseases such as Parkinson's.

Nurr1 agonist 7 (compound 110) is an agonist targeting the Nurr1 receptor, exhibiting an EC₅₀ of 0.12 μM ^[1].

Digoxigenin bisdigitoxoside (Bisdigoxigenin) is a digoxigenin metabolite with anticancer activity and cytotoxicity.

Nurr1 agonist 9 (Compound 36) acts as an agonist for Nurr1, with an EC₅₀ of 0.090 µM and a Kd of 0.17 µM. It activates Nurr1 homodimers (NurRE, EC₅₀ = 0.094 µM) and Nurr1-RXR heterodimers (DR5, EC₅₀ = 0.165 µM). This compound induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in Parkinson's disease organoid models and can penetrate the human brain endothelial cell barrier.

Nurr1 agonist 12 (Compound 37) acts as an agonist of the nuclear receptor-related protein 1 (Nurr1), enhancing its transcriptional activity with an EC₅₀ of 0.06 μM. It stimulates human response elements NBRE, NurRE, and DR5 with EC₅₀ values of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Additionally, Nurr1 agonist 12 induces the expression of neurotrophic genes regulated by Nurr1, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). The compound also demonstrates neuroprotective effects against neurotoxicity caused by Paraquat.

THPN is a Nur77 agonist. It also induces autophagy in melanoma cell lines.

Nurr1 Agonist 14 (Compound 32) is a Nurr1 agonist with an EC₅₀ of 0.09 μM for Nurr1. It exhibits significant neuroprotective activity without being hindered by residual DHODH inhibition. This compound can upregulate neuroprotective genes in dopaminergic neurons, such as SOD2, SESN3, BIRC5, XIAP, FLRT2, and CRMP4. Nurr1 Agonist 14 is useful for studying neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and multiple sclerosis (MS).

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC₅₀ of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

NR4A agonist-2, derived from the design of Vidofludimus, is a selective pan-NR4A agonist with a dissociation constant (Kd) of 0.10 μM for NR4A1 and half-maximal effective concentrations (EC₅₀) of 0.098 μM, 0.092 μM, and 0.09 μM for Nur77, Nurr1, and NOR-1, respectively. It exhibits 47-fold selectivity for DHODH and demonstrates no cytotoxic activity at concentrations up to 10 μM. NR4A agonist-2 acts by binding to a specific surface pocket in the ligand-binding domain of Nurr1, inhibiting Nurr1 homodimer formation and activating response elements such as NBRE, NurRE, and DR5, thus robustly inducing the expression of neuroprotective genes like BDNF and SOD2. This compound holds potential for research in neurodegenerative diseases including Parkinson's disease, dementia, and multiple sclerosis.