2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Nuclear Hormone Receptor 4A/NR4A
  5. Nurr1/NR4A2 Isoform

Nurr1/NR4A2

 

Nurr1/NR4A2 Related Products (17):

Cat. No. Product Name Effect Purity
  • HY-B1322A
    Amodiaquine
    		Agonist 99.92%
    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.
  • 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.
  • HY-B1322B
    Amodiaquine dihydrochloride
    		Agonist 99.97%
    Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
  • 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.
  • HY-19808
    C-DIM12
    		Modulator 98.01%
    C-DIM12 is a potent, orally active Nurr1 modulator. 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.
  • HY-179528
    DIM-3,5-Cl2
    		Antagonist 99.18%
    DIM-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.
  • HY-180576
    Nurr1/RXR agonist 1
    		Inhibitor
    Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with Ks of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research.
  • HY-110274
    IP7e
    		Activator 99.72%
    IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC50 value of 3.9 nM.
  • HY-W677684
    Nurr1 agonist 2
    		Agonist 98.03%
    Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC50: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a Kd value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression.
  • HY-132909
    Nurr1 inverse agonist-1
    		Agonist 98.83%
    Nurr1 inverse agonist-1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
  • HY-173025
    Nurr1 agonist 12
    		Agonist 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.
  • HY-175352
    Nurr1 agonist 14
    		Agonist 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.
  • HY-163801
    Nurr1 agonist 9
    		Agonist
    Nurr1 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.
  • HY-174340
    Nurr1 agonist 13
    		Agonist
    Nurr1 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.
  • HY-163802
    Nurr1 agonist 10
    		Agonist
    Nurr1 agonist 10 (compound 37) is a potent Nurr1 agonist with an EC50 value of 40 nM. Nurr1 agonist 10 has the potential for the research of Parkinson’s and Alzheimer’s disease.
  • HY-149608
    Nurr1 agonist 5
    		Agonist
    Nurr1 agonist 5 (compound 5o) is a neuroprotective transcription factor Nurr1 agonist with a Kd of 0.5 μM and an EC50 of 3 μM.
  • HY-181588
    NR4A agonist-2
    		Agonist
    NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis.