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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
TAK633, TAK 633, Revestive, Gattex, ALX-0600, ALX0600
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
Cited
Dothiorelone G, Csn-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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CitedDIM-C-pPhOH
CDIM8
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
isoxazolo-pyridinone 7e, IP-7e, IP 7e
T27620500164-74-9
IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.
- $48
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Amodiaquine dihydrochloride dihydrate
Amodiaquine hydrochloride, Amodiaquin 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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NOT Receptor Modulator 1
2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol
T122471015231-98-7
NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.
- $48
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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.
- $88
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Nur77 modulator 1
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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DIM-C-pPhOCH3
C-DIM5
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 agonist 8
T81632360778-55-8In house
Nurr1 agonist 8 is a low-affinity Nurr1 agonist that can be used to study neurological diseases such as Parkinson's.
- $40
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Nurr1 agonist 7
T81633228707-95-7
Nurr1 agonist 7 (compound 110) is an agonist targeting the Nurr1 receptor, exhibiting an EC50 of 0.12 μM [1].
- $44
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Digoxigenin bisdigitoxoside
Bisdigoxigenin
T862125297-05-2
Digoxigenin bisdigitoxoside (Bisdigoxigenin) is a digoxigenin metabolite with anticancer activity and cytotoxicity.
- $1,130
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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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Nurr1 agonist 9
T210048
Nurr1 agonist 9 (Compound 36) acts as an agonist for Nurr1, with an EC50 of 0.090 µM and a Kd of 0.17 µM. It activates Nurr1 homodimers (NurRE, EC50 = 0.094 µM) and Nurr1-RXR heterodimers (DR5, EC50 = 0.165 µM). This compound induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in Parkinson's disease organoid models and can penetrate the human brain endothelial cell barrier.
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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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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 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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