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Endocrinology/HormonesNR4A
Nuclear Hormone Receptor 4A (NR4A) is a class of orphan nuclear receptors comprising NR4A1, NR4A2, and NR4A3. NR4A receptors are expressed in diverse cell types, participating in the regulation of cell proliferation, differentiation, apoptosis, and metabolism. NR4A receptors modulate gene transcription by binding to specific DNA sequences. Within the immune system, NR4A receptors contribute to regulating T-cell activation and immune responses. Metabolically, NR4A receptors influence lipid metabolism and glucose homeostasis by regulating gene expression in adipocytes and the liver. Abnormal expression of NR4A receptors is associated with various diseases, including cardiovascular disorders, diabetes mellitus, and cancer.
Teduglutide
T35337197922-42-2
Teduglutide (ALX-0600) is a glucagon-like peptide-2 analog that increases intestinal absorption by promoting mucosal growth and reducing mucosal degradation, improving intestinal recovery. It is used in the study of short bowel syndrome (SBS). Teduglutide activates NR4a1/nur77 expression and FXR signaling, alleviating intestinal dysfunction in mice and improving lung injury, making it useful for studying metabolic and cardiovascular diseases.
- $77
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Broussochalcone A
T7259499217-68-2
Broussochalcone A is a natural antioxidant and xanthine oxidase inhibitor (IC50 = 2.21 μM) that scavenges free radicals, inhibits iron-induced lipid peroxidation, and reduces nitric oxide synthesis in LPS-activated macrophages. Broussochalcone A induces apoptosis in human renal carcinoma cells by increasing ROS levels and activating the FOXO3 signaling pathway. Broussochalcone A is also a novel NR4A1 inhibitor that induces apoptosis in pancreatic cancer cells through NR4A1-dependent pathways.
- $198
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Amodiaquine
T838186-42-0
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
- $44
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Cytosporone B
T3976321661-62-5
Cytosporone B (Dothiorelone G) is a naturally occurring agonist of the nuclear orphan receptor Nur77/NR4A1 (EC50=0.278 nM).
- $39
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DIM-C-pPhOH
T4400151358-47-3
DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.
- $37
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IP7e
T27620500164-74-9
IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.
- $117
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Amodiaquine dihydrochloride dihydrate
T03816398-98-7
Amodiaquine dihydrochloride dihydrate (Amodiaquine hydrochloride) is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties.
- $33
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TMPA
T131731258275-73-8
TMPA is a nuclear receptor Nur77 and LKB1 interaction antagonist.
- $73
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Nurr1 agonist 2
T77549742058-34-0
Nurr1 agonist 2 is a Nurr1 agonist with an EC50 value of 0.07 μM. Nurr1 agonist 2 increases the mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand-binding domain (LBD) with a Kd of 0.14 μM. Nurr1 agonist 2 can be used to study parkinsonism.
- $147
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Nur77 modulator 1
T401302469975-55-9
Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.
- $58
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4-PQBH
T614282243355-51-1
4-PQBH is a potent Nur77-binding agent with antitumour activity.4-PQBH inhibits xenograft tumours through Nur77-mediated endoplasmic stress and autophagy by broadly inducing cysteoaspartase-independent cytoplasmic vacuolisation and parapetaloid ptosis.4-PQBH is used in the study of hepatocellular carcinoma.4-PQBH is a potent Nur77-binding agent with antitumour activity.
- $69
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C-DIM12
T3106178946-89-9
C-DIM12 induced expression of Nurr1-regulated genes. C-DIM12 increased expression of transfected human Nurr1, induced Nurr1 protein expression in primary dopaminergic neurons and enhanced neuronal survival from exposure to 6-OHDA.
- $38
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DIM-C-pPhOCH3
T439733985-68-1
DIM-C-pPhOCH3 (C-DIM5) is a Nerve Growth Factor-Induced Bα (NGFI-Bα, Nur77) agonist
- $30
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DIM-C-pPhCO2Me
T5196151358-48-4
DIM-C-pPhCO2Me is an antagonist of nuclear receptor 4A1 (NR4A1).
- $30
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Nurr1 inverse agonist-1
T780492758673-07-1
Nurr1 Inverse Agonist-1 is an inverse agonist for the neuroprotective transcription factor Nurr1, serving as a research tool.
- $142
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ST-CY14
TP3109
ST-CY14 is an inhibitor of the Nur77-PPARγ interaction with an EC50 of 3.15 μM. It binds to Nur77 (Kd=32 nM) to prevent its ubiquitination and degradation by PPARγ, reducing fatty acid uptake and mitochondrial respiration, and inhibiting the transcription of CD36 and FABP4. ST-CY14 suppresses proliferation and migration of MCF7 and MDA-MB-231 cancer cells and impedes tumor growth and bone metastasis in mouse models.
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THPN
T24880100079-26-3
THPN is a Nur77 agonist. It also induces autophagy in melanoma cell lines.
- $1,520
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Nurr1 agonist 12
T206188
Nurr1 agonist 12 (Compound 37) acts as an agonist of the nuclear receptor-related protein 1 (Nurr1), enhancing its transcriptional activity with an EC50 of 0.06 μM. It stimulates human response elements NBRE, NurRE, and DR5 with EC50 values of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Additionally, Nurr1 agonist 12 induces the expression of neurotrophic genes regulated by Nurr1, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). The compound also demonstrates neuroprotective effects against neurotoxicity caused by Paraquat.
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Nur77 modulator 2
T624062055829-03-1
Nur77 modulator 2 is a Nur77 regulator with a Kd value of 0.35 μM. Nur77 modulator 2 is also a potent, orally active inhibitor of inflammation. nur77 modulator 2 regulates Nur77 co-localization in mitochondria.
- $1,520
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Amoitone B
T856461257228-26-4
Amoitone B, a cystosporone B derivative, functions as an NR4A1 agonist and exhibits anticancer activity [1].
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Nur77 agonist-1
T2069542899254-71-6
Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. It induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, while decreasing GPX4 protein expression. Nur77 agonist-1 binds with affinity to the ligand binding domain of Nur77, with a KD of 13.80 μM. It demonstrates significant antiproliferative activity against various breast cancer cells (IC50: 2.15-3.26 μM) and exhibits low cytotoxicity towards normal cells. This compound is useful for breast cancer research.
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Nur77 modulator 4
T205370
Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on 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, leading to apoptosis. This compound is applicable in cancer research.
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Amodiaquine hydrochloride
T2224269-44-3
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, is an antimalarial agent that also acts as a potent oral histamine N-methyltransferase inhibitor with a K i value of 18.6 nM. Additionally, it functions as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, demonstrating anti-inflammatory effects [1] [2] [3] [4] [5].
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Nur77 antagonist 1
T870462378780-25-5
Nur77 antagonist 1 (Compound ja) is a selective Nur77 antagonist (K D SPR Nur77 = 91 nM) that induces cancer cell apoptosis and exhibits excellent antitumor activity against triple-negative breast cancer (TNBC) cells [1].
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