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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DIM-C-pPhOCH3
0 ImagesDIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
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DIM-3,5-Cl2
0 ImagesDIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with KD values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively. DIM-3,5-Cl2 acts as an inverse agonist to downregulate pro-oncogenic and proendometriotic gene products, and as an agonist to enhance NR4A1/2/Sp1/Sp4-mediated CD71 transactivation. DIM-3,5-Cl2 induces ferroptosis via ROS formation, lipoperoxidation, MDA production, and reduced GPX4, SLC7A11 expression. DIM-3,5-Cl2 induces apoptosis via PARP and caspase-3 cleavage, reduced BCL-2 expression, and inhibits cancer cell viability. DIM-3,5-Cl2 can be used for the research of triple negative breast cancer, endometriosis, and colorectal cancer.
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Nurr1 agonist 12
0 ImagesCat. No.: HY-173025Purity: 99.62%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.
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Nurr1 agonist 7
0 ImagesNurr1 agonist 7 (compound 110) is a Nurr1 agonist with an EC50 value of 0.12 μM.
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4-PQBH
0 Images4-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.
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Amoitone B
0 ImagesAmoitone B, a derivative of cystosporone B, is an agonist of NR4A1. Amoitone B has anticancer activity.
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BI1071
0 ImagesCat. No.: HY-111837Purity: 98.93%BI1071 is an orally active Nur77-Bcl-2 apoptotic pathway modulator. BI1071 can bind to Nur77-LBD protein with a Kd of 0.17 μM. BI1071 can activate Nur77 signaling and induce apoptosis by translocating to mitochondria where it interacts with Bcl-2. BI1071 can inhibit tumor growth in SW620 xenograft mice model. BI1071 can be used for research of colon cancer.
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Nurr1 agonist 4
0 ImagesNurr1 agonist 4 (compound 8) is a high-affinity Nurr1 agonist with EC50 of 2.1 μM.
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Amodiaquine dihydrochloride dihydrate (Standard)
0 ImagesSynonyms: Amodiaquin dihydrochloride dihydrate (Standard)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.
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Prostaglandin E2-biotin
0 ImagesCat. No.: HY-157807CAS No.: 2641624-60-2Prostaglandin E2-biotin is a prostaglandin analog. Prostaglandin E2-biotin can be used for research of Nurr1-related disease, such as cancer and autoimmune disease.
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Nurr1 agonist 14
0 ImagesCat. No.: HY-175352Purity: 99.42%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.
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NOT Receptor Modulator 1
0 ImagesNOT Receptor Modulator 1 is a nuclear receptor Nurr-1/NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
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Teduglutide-Leu(13C6,15N) sodium
0 ImagesCat. No.: HY-P1624S1Synonyms: ALX-0600-Leu(13C6,15N) sodiumTeduglutide-Leu(13C6,15N) (ALX-0600-Leu(13C6,15N)) sodium is the 13C- and 15N-labeled Teduglutide (HY-P1624). 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.
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ST-CY14
0 ImagesCat. No.: HY-P10873ST-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.
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Nurr1 agonist 6
0 ImagesCat. No.: HY-149609CAS No.: 3033875-47-4Nurr1 agonist 6 (compound 13) is a Nurr1 agonist with Kd value of 1.5 μM and EC50 value of 3 μM.
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Digoxigenin bisdigitoxoside
0 ImagesDigoxigenin 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.
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PROTAC IKKβ/NR4A1 degrader-1
0 ImagesCat. No.: HY-179112CAS No.: 2826215-20-5PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).
