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-113827
    THPN
    		Agonist 98.00%
    THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma.
    THPN
  • HY-W270810
    NR4A agonist-1
    		Agonist 99.93%
    NR4A agonist-1, a fatty acid mimetic (FAM), is a potent NR4A agonist. NR4A agonist-1 exhibits high agonist potency on NR4A receptors Nurr1, Nur77, and NOR-1, with EC50s of 0.09 μM, 0.04 μM, and 0.15 μM, respectively.
    NR4A agonist-1
  • HY-131364
    Nur77 modulator 1
    		98.61%
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
    Nur77 modulator 1
  • HY-157026
    Nurr1 agonist 7
    		Agonist 99.90%
    Nurr1 agonist 7 (compound 110) is a Nurr1 agonist with an EC50 value of 0.12 μM.
    Nurr1 agonist 7
  • HY-U00429
    NOT Receptor Modulator 1
    		Modulator 98.61%
    NOT Receptor Modulator 1 is a nuclear receptor Nurr-1/NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
    NOT Receptor Modulator 1
  • HY-160498
    Amoitone B
    		Agonist 98.50%
    Amoitone B, a derivative of cystosporone B, is an agonist of NR4A1. Amoitone B has anticancer activity.
    Amoitone B
  • HY-157807
    Prostaglandin E2-biotin
    		≥99.0%
    Prostaglandin E2-biotin is a prostaglandin analog. Prostaglandin E2-biotin can be used for research of Nurr1-related disease, such as cancer and autoimmune disease.
    Prostaglandin E2-biotin
  • HY-149867
    Nurr1 agonist 4
    		Agonist 98.74%
    Nurr1 agonist 4 (compound 8) is a high-affinity Nurr1 agonist with EC50 of 2.1 μM.
    Nurr1 agonist 4
  • HY-P10873
    ST-CY14
    		Ligand
    ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models.
    ST-CY14
  • HY-149609
    Nurr1 agonist 6
    		Agonist
    Nurr1 agonist 6 (compound 13) is a Nurr1 agonist with Kd value of 1.5 μM and EC50 value of 3 μM.
    Nurr1 agonist 6
  • HY-131486
    Digoxigenin bisdigitoxoside
    		Control
    Digoxigenin bisdigitoxoside is an anticancer agent and an active derivative of cardiac glycosides. Cardiac glycosides exert their apoptotic effects through the Nur77-dependent apoptotic pathway. Digoxigenin bisdigitoxoside is cytotoxic.
    Digoxigenin bisdigitoxoside
  • HY-173025
    Nurr1 agonist 12
    		Agonist
    Nurr1 agonist 12 (Compound 37) is the agonist for nuclear receptor-associated protein 1 (Nurr1) that activates the transcriptional activity of Nurr1 with an EC50 of 0.06 μM. Nurr1 agonist 12 activates the human response elements NBRE, NurRE, and DR5 with EC50 of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Nurr1 agonist 12 induces the expression of Nurr1-regulated neurotrophic genes, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). Nurr1 agonist 12 exhibits neuroprotective efficacy against Paraquat-induced neurotoxicity.
    Nurr1 agonist 12
  • HY-162786
    Nurr1 agonist 11
    		Agonist
    Nurr1 agonist 11 (compound 53) is a selective and potent Nurr1 agonist with an IC50 of 26 µM. Nurr1 agonist 11 has the ability to cross a cellular model of the blood-brain-barrier (BBB) .
    Nurr1 agonist 11
  • HY-138967
    BRF110
    BRF110 is the selective, orally active rexinoid for Nurr1-RXRα, that selectively activates the Nurr1-RXRα heterodimer with an EC50 of 0.9 μM in SH-SY5Y. BRF110 upregulates the expression of BDNF, exhibits neuroprotective activity against MPP+ induced toxicity. BRF110 can cross blood-brain barrier.
    BRF110
  • HY-P1624A
    Teduglutide TFA
    		Activator
    Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA 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 TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
    Teduglutide TFA
  • HY-170849
    Nur77 modulator 4
    		Inducer
    Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in 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, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
    Nur77 modulator 4
  • HY-115923
    Nur77 modulator 2
    Nur77 modulator 2, a Nur77 modulator (Kd of 0.35 μM), is a potent and orally active inflammation inhibitor. Nur77 modulator 2 modulates the colocalization of Nur77 at mitochondria.
    Nur77 modulator 2
  • HY-155490
    Nur77 antagonist 1
    		Antagonist
    Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells.
    Nur77 antagonist 1
  • HY-163801
    Nurr1 agonist 9
    		Agonist
    Nurr1 agonist 9 (Compound 36) is an agonist for Nurr1 with an EC50 of 0.090 µM and a Kd of 0.17 µM. Nurr1 agonist 9 activates the Nurr1 homodimer (NurRE, EC50=0.094 µM) and the Nurr1-RXR heterodimer (DR5, EC50=0.165 µM). Nurr1 agonist 9 induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in organoid Parkinson's Disease model. Nurr1 agonist 9 is human brain endothelial cell barrier prmeable.
    Nurr1 agonist 9
  • HY-169906
    Anticancer agent 257
    		Modulator
    Anticancer agent 257 (compound of formula (I)) is an anticancer agent with Nur77 and Nurrl modulating effects.
    Anticancer agent 257
Cat. No. Product Name / Synonyms Application Reactivity
Nuclear Hormone Receptor 4A/NR4A Isoform Comparison

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