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].
References:
- [1]. Wang M, et al. Brain nuclear receptors and cardiovascular function[J]. Cell & Bioscience, 2023, 13(1): 14. [Content Brief]
- [2]. Ye F, et al. Recruitment of the CoREST transcription repressor complexes by Nerve Growth factor IB-like receptor (Nurr1/NR4A2) mediates silencing of HIV in microglial cells[J]. PLoS Pathogens, 2022, 18(7): e1010110. [Content Brief]
- [3]. Yu H, et al. Dual role of NR4A1 in porcine ovarian granulosa cell differentiation and granulosa-lutein cell regression in vitro. Theriogenology. 2023 Mar 1;198:292-304. [Content Brief]
- [4]. Yang Y, et al. The orphan nuclear receptor NR4A1 attenuates oxidative stress-induced β cells apoptosis via up-regulation of glutathione peroxidase 1. Life Sci. 2018 Jun 15;203:225-232. [Content Brief]
Nuclear Hormone Receptor 4A/NR4A Isoform Specific Products
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Nuclear Hormone Receptor 4A/NR4A Related Products (70)
Related Products (70)
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Antibodies (4)
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Nuclear Hormone Receptor 4A/NR4A Isoform Comparison
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Nur77 antagonist 2
0 ImagesCat. No.: HY-179033Nur77 antagonist 2 (Compound 12b) is an orally active Nur77 antagonist with a KD value of 0.42 μM. Nur77 antagonist 2 exhibits proliferative activity on liver cancer cells. Nur77 antagonist 2 stabilizes Nur77 by inhibiting its ubiquitin-proteasomal degradation, leading to Nur77-dependent apoptosis via the ASK1-JNK/p38 pathway. Nur77 antagonist 2 inhibits tumor growth in the HCCLM3 xenograft model. Nur77 antagonist 2 can be used for the study of hepatocellular carcinoma (HCC).
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Nurr1 agonist 11
0 ImagesCat. No.: HY-162786CAS No.: 1090335-04-8Nurr1 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) .
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DdBIC
0 ImagesCat. No.: HY-180786CAS No.: 3085711-53-8DdBIC is a pyroptosis inducer. DdBIC binds to Nur77 and triggers its translocation to mitochondria, activates SDHA to deplete succinyl-CoA, disrupts heme homeostasis, induces electron leakage, and elicits mitochondrial ROS production. DdBIC induces mitochondrial ROS that oxidatively activates OMA1, promotes OPA1 cleavage and its release into the cytoplasm, activates the integrated stress response via PERK, and ultimately activates granzyme B to cleave GSDMC. DdBIC can be used for the study of melanoma.
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CM002
0 ImagesCat. No.: HY-184895CM002 is a circadian clock activator. CM002 inhibits the lineage commitment and terminal differentiation of preadipocytes by activating the circadian clock, thereby blocking the adipogenesis process driven by Wnt signaling-mediated transcriptional induction. CM002 attenuates lipid storage in a clock-dependent manner via inhibition of the lipogenic program in mature adipocytes. CM002 enhances circadian clock output across various adipose depots in both lean and obese mice through BMAL1/CLOCK-dependent metabolic reprogramming, inhibits adipocyte development and hypertrophy, and improves insulin sensitivity. CM002 can be used in research on obesity and type 2 diabetes.
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BRF110
0 ImagesCat. No.: HY-138967CAS No.: 2095489-35-1BRF110 is an orally active, blood-brain barrier-penetrant Nurr1-RXRα heterodimer activator with an EC50 of 0.9 μM in human systems. BRF110 increases the mRNA level of BDNF, upregulates the transcription of TH, AADC and GCH1 to elevate striatal dopamine levels. BRF110 exhibits neuroprotective activity against MPP+-induced cytotoxicity. BRF110 prevents dopaminergic neuron death, protects nerve cells from toxic damage, and improves motor coordination in mouse models. BRF110 can be used in research related to Parkinson's disease.
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Teduglutide TFA
0 ImagesCat. No.: HY-P1624ASynonyms: ALX-0600 TFATeduglutide 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.
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Nur77 modulator 4
0 ImagesCat. No.: HY-170849Nur77 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 .
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Nur77 modulator 2
0 ImagesCat. No.: HY-115923CAS No.: 2055829-03-1Nur77 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.
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Nur77 antagonist 1
0 ImagesCat. No.: HY-155490CAS No.: 2378780-25-5Nur77 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.
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Nur77 modulator 6
0 ImagesCat. No.: HY-183758Nur77 modulator 6 is a Nur77 modulator with a Kd of 0.40 μM. Nur77 modulator 6 functionally modulates Nur77 to induce mitotic arrest and apoptosis in colorectal tumor cells. Nur77 modulator 6 suppresses colorectal cancer cell proliferation via Nur77-dependent mitotic arrest induction. Nur77 modulator 6 exhibits anti-proliferative activity against colorectal tumor cells. Nur77 modulator 6 can be used for the research of colorectal cancer.
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Nurr1 agonist 9
0 ImagesCat. No.: HY-163801Nurr1 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.
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Anticancer agent 257
0 ImagesCat. No.: HY-169906CAS No.: 2891997-46-7Anticancer agent 257 (compound of formula (I)) is an anticancer agent with Nur77 and Nurrl modulating effects.
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Nurr1 agonist 13
0 ImagesCat. No.: HY-174340Nurr1 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.
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Amodiaquine-d10 hydrochloride
0 ImagesCat. No.: HY-B1322AS1Synonyms: Amodiaquin-d10Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). 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.
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SR10098
0 ImagesCat. No.: HY-W193645CAS No.: 850705-30-5SR10098 is a benzimidazole-based Nurr1 activator with an EC50 of 24 nM against full-length Nurr1. SR10098 does not directly bind to the ligand-binding domain of Nurr1, regulates transcription via a Nurr1-independent pathway, and exhibits no significant cytotoxicity. SR10098 can be used in studies of Nurr1-related diseases, such as Alzheimer's disease and Parkinson's disease.
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Nur77 modulator 3
0 ImagesNur77 modulator 3 is a Nur77 modulator. Nur77 modulator 3 induces Nur77 expression, inhibits hepatic stellate cells (HSCs) activation, and reduces extracellular matrix (ECM) deposition. Nur77 modulator 3 enhances Nur77-denpendent autophagic flux and significantly inhibits the mTORC1 signaling pathway. Nur77 modulator 3 ameliorates HSCs activation, inflammation and hepatic fibrosis in vivo.
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Nur77 agonist-1
0 ImagesCat. No.: HY-173408CAS No.: 2899254-71-6Nur77 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.
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BIM5078
0 ImagesCat. No.: HY-119971CAS No.: 337506-43-1
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Anticancer agent 258
0 ImagesCat. No.: HY-169907CAS No.: 2891984-12-4Anticancer agent 258 is an imidazo [1,2-B][1,2,4] triazol derivative. Anticancer agent 258 regulates the activity of nuclear receptors. Anticancer agent 258 has an EC50 of 63 nM against Nurr in N2A cells. Anticancer agent 258 has IC50 of 0.1 pM for Nur77 in HEK293 cells. Anticancer agent 258 can be used in the study of cancer, metabolic diseases and neurological disorders.
