Nuclear Hormone Receptor 4A/NR4A Agonist

Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC₅₀ of 0.278 nM.

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.

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.

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i 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.

4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC₅₀ values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [³H]-CQ competition assay and TR-FRET assay, respectively. The EC₅₀ of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC₅₀ in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP⁺ or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease.

Nurr1 inverse agonist-1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.

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 K_d 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.

NR4A agonist-1, a fatty acid mimetic (FAM), is a potent NR4A agonist. NR4A agonist-1 exhibits high agonist potency on NR4A receptors Nurr1, Nur77, and NOR-1, with EC₅₀s of 0.09 μM, 0.04 μM, and 0.15 μM, respectively.

ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC₅₀ of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer.

DIM-C-pPhOCH₃ is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.

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.

THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a K_d of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma.

Nurr1 agonist 7 (compound 110) is a Nurr1 agonist with an EC₅₀ value of 0.12 μM.

Amoitone B, a derivative of cystosporone B, is an agonist of NR4A1. Amoitone B has anticancer activity.

Nurr1 agonist 4 (compound 8) is a high-affinity Nurr1 agonist with EC₅₀ of 2.1 μM.

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.

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.

Nurr1 agonist 6 (compound 13) is a Nurr1 agonist with K_d value of 1.5 μM and EC₅₀ value of 3 μM.

Nurr1 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) .

Nurr1 agonist 9 (Compound 36) is an agonist for Nurr1 with an EC₅₀ of 0.090 µM and a K_d 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.