2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Nuclear Hormone Receptor 4A/NR4A

Nuclear Hormone Receptor 4A/NR4A

Nuclear Hormone Receptor 4A; Nerve Growth Factor IB-like Receptor

Nuclear Hormone Receptor 4A (NR4A) belongs to the nuclear receptor (NR) superfamily and comprises three members: NR4A1 (Nur77), NR4A2 (Nurr1), and NR4A3 (Nor1), all of which are classified as "orphan receptors" (without a clearly defined natural ligand). NR4A plays pivotal roles in various cell types, including proliferation, apoptosis, DNA repair, cellular stress, memory, endocrinology, neuronal signaling, as well as hematopoietic, immune, and metabolic processes. Furthermore, NR4A is implicated in the pathogenesis and progression of numerous diseases, such as obesity, vascular diseases, inflammation, metabolic disorders, and neurodegenerative diseases[1][2][3][4].

Nuclear Hormone Receptor 4A/NR4A Isoform Specific Products:

Nuclear Hormone Receptor 4A/NR4A Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2148
    Cytosporone B
    		Agonist 99.23%
    Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
    Cytosporone B
  • HY-112055
    DIM-C-pPhOH
    		Antagonist 99.05%
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
    DIM-C-pPhOH
  • HY-B1322A
    Amodiaquine
    		Agonist 99.98%
    Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine
  • HY-P1624
    Teduglutide
    		Activator 99.94%
    Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
    Teduglutide
  • HY-B1322
    Amodiaquine dihydrochloride dihydrate
    		Agonist 99.92%
    Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine dihydrochloride dihydrate
  • HY-175352
    Nurr1 Agonist 14
    		Agonist
    Nurr1 Agonist 14 (Compound 32) is a Nurr1 agonist with an EC50 of 0.09  μM for Nurr1. Nurr1 Agonist 14 has significant neuroprotective activity with no influence of residual DHODH inhibition. Nurr1 Agonist 14 upregulates neuroprotective genes including SOD2, SESN3, BIRC5, XIAP, FLRT2 and CRMP4 in dopaminergic neurons. Nurr1 Agonist 14 can be used for neurodegenerative diseases such as Alzheimer′s disease (AD), Parkinson′s disease (PD) and multiple sclerosis (MS) research.
    Nurr1 Agonist 14
  • HY-174340
    Nurr1 agonist 13
    		Agonist
    Nurr1 agonist 13 (Compound 1) is a potent nuclear receptor related 1 (Nurr1, NR4A2) agonist with an EC50 value of 0.06 μM. Nurr1 agonist 13 is promising for research of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and multiple sclerosis.
    Nurr1 agonist 13
  • HY-173408
    Nur77 agonist-1
    		Agonist
    Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research.
    Nur77 agonist-1
  • HY-18555
    TMPA
    		Antagonist 98.40%
    TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.
    TMPA
  • HY-B1322B
    Amodiaquine dihydrochloride
    		Agonist 99.97%
    Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine dihydrochloride
  • HY-19808
    C-DIM12
    		Modulator 98.01%
    C-DIM12 is a potent, orally active Nurr1 modulator. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study.
    C-DIM12
  • HY-155659
    4A7C-301
    		Agonist 99.86%
    4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease.
    4A7C-301
  • HY-112056
    DIM-C-pPhCO2Me
    		Antagonist 99.47%
    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research.
    DIM-C-pPhCO2Me
  • HY-W677684
    Nurr1 agonist 2
    		Agonist 98.03%
    Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC50: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a Kd value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression.
    Nurr1 agonist 2
  • HY-110274
    IP7e
    		Activator 99.65%
    IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC50 value of 3.9 nM.
    IP7e
  • HY-117469
    Triptohypol C
    Triptohypol C, a Tripterin (HY-13067) derivative, is a potent Nur77-targeting anti-inflammatory agent with an Kd value of 0.87 μM. Triptohypol C inhibits inflammatory response by promoting the interactions of Nur77 with TRAF2 and p62/SQSTM1.
    Triptohypol C
  • HY-111492
    DIM-C-pPhOCH3
    		Agonist 99.65%
    DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
    DIM-C-pPhOCH3
  • HY-115901
    4-PQBH
    		99.14%
    4-PQBH is a potent Nur77 binder (KD=1.17 μM). 4-PQBH extensively induces caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy. 4-PQBH can be used for cancer research.
    4-PQBH
  • HY-132909
    Nurr1 inverse agonist-1
    		Agonist 99.79%
    Nurr1 inverse agonist-1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
    Nurr1 inverse agonist-1
  • HY-159779
    NR-V04
    		Degrader
    NR-V04 is a PROTAC based NR4A1 degrader (Red: NR4A1 inhibitor (HY-13067), black: linker, Blue: E3 ligase ligand).
    NR-V04
Cat. No. Product Name / Synonyms Application Reactivity
Nuclear Hormone Receptor 4A/NR4A Isoform Comparison

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