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

Nuclear Hormone Receptor 4A/NR4A

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 Related Products (45):

Cat. No. Product Name Effect Purity
  • 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[1][2][3][4].
  • 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[1].
  • 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[1][2][3][4].
  • HY-N2148
    Cytosporone B Agonist
    Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
  • 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[1][2][3][4].
  • 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[1].
  • 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[1].
  • 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[1].
  • HY-B1322R
    Amodiaquine (dihydrochloride dihydrate) (Standard) Agonist
    Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. 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[1][2][3][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[1].
  • 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[1].
  • 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[1].
  • 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[1].
  • 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[1][2].
  • HY-115901
    4-PQBH 99.08%
    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[1].
  • 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) [1].
  • HY-N2148R
    Cytosporone B (Standard) Agonist
    Cytosporone B (Standard) is the analytical standard of Cytosporone B. This product is intended for research and analytical applications. Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
  • HY-19808
    C-DIM12 Antagonist 98.32%
    C-DIM12 is a potent, orally active Nurr1 antagonist. 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[1][2][3].
  • HY-159779
    NR-V04 Degrader
    NR-V04 is a PROTAC based NR4A1 degrader (Red: NR4A1 inhibitor (HY-13067), black: linker, Blue: E3 ligase ligand)[1].
  • 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[1][2][3][4].