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ligand binding domain (LBD)

" in MedChemExpress (MCE) Product Catalog:

27

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1322A
    Amodiaquine
    Maximum Cited Publications
    10 Publications Verification

    Amodiaquin

    		 Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    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
  • HY-B1322B
    Amodiaquine dihydrochloride
    Maximum Cited Publications
    10 Publications Verification

    Amodiaquin dihydrochloride

    		 Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    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 .
    Amodiaquine dihydrochloride
  • HY-B1322
    Amodiaquine dihydrochloride dihydrate
    Maximum Cited Publications
    10 Publications Verification

    Amodiaquin dihydrochloride dihydrate

    		 Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    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 dihydrate
  • HY-B1322AS
    Amodiaquine-d10

    		Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    Amodiaquine-d10 is the deuterium labeled Amodiaquine. 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-d10
  • HY-120210
    XY018

    		ROR Inflammation/Immunology Cancer
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
    XY018
  • HY-111254
    GQ-16

    		PPAR Metabolic Disease
    GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain .
    GQ-16
  • HY-B1322AS1
    Amodiaquine-d10 hydrochloride

    Amodiaquin-d10

    		 Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Isotope-Labeled Compounds Infection Neurological Disease Inflammation/Immunology
    Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). 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-d10 hydrochloride
  • HY-B1322AR
    Amodiaquine (Standard)

    		Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    Amodiaquine (Standard) is the analytical standard of Amodiaquine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1322BR
    Amodiaquine dihydrochloride (Standard)

    		Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    Amodiaquine (dihydrochloride) (Standard) is the analytical standard of Amodiaquine (dihydrochloride). This product is intended for research and analytical applications. 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 .
    Amodiaquine dihydrochloride (Standard)
  • HY-B1322R
    Amodiaquine dihydrochloride dihydrate (Standard)

    Amodiaquin dihydrochloride dihydrate (Standard)

    		 Nuclear Hormone Receptor 4A/NR4A Reference Standards Parasite Histone Methyltransferase Infection Neurological Disease Inflammation/Immunology
    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 .
    Amodiaquine dihydrochloride dihydrate (Standard)
  • HY-162738
    JMV6944

    		Cytochrome P450 Ligands for Target Protein for PROTAC Cancer
    JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704) .
    JMV6944
  • HY-170874
    PPARγ modulator-2

    		PPAR Metabolic Disease
    PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
    PPARγ modulator-2
  • HY-132205
    DS45500853

    		Estrogen Receptor/ERR Metabolic Disease
    DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
    DS45500853
  • HY-143201
    DS20362725

    		Estrogen Receptor/ERR Metabolic Disease
    DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
    DS20362725
  • HY-137818
    SR19881

    		Estrogen Receptor/ERR Cardiovascular Disease
    SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively .
    SR19881
  • HY-141551
    GNE-274

    		Estrogen Receptor/ERR Cancer
    GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
    GNE-274
  • HY-136242
    UT-34

    		Estrogen Receptor/ERR Endocrinology Cancer
    UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
    UT-34
  • HY-121372
    Lactandrate

    		Estrogen Receptor/ERR Cancer
    Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
    Lactandrate
  • HY-W677684
    Nurr1 agonist 2

    		Nuclear Hormone Receptor 4A/NR4A Others
    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 .
    Nurr1 agonist 2
  • HY-122742
    HBT1

    		iGluR Neurological Disease
    HBT1 is a potent α-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor (AMPA-R) potentiator. HBT1 bonds with S518 in the ligand-binding domain (LBD) of AMPA-R in a glutamate-dependent manner. HBT1 did not show remarkable bell-shaped response in brain-derived neurotrophic factor (BDNF) production in primary neurons .
    HBT1
  • HY-173393
    LXRα agonist 1

    		LXR Cancer
    LXRα agonist 1 (Compound 40) is a selective LXRα agonist (EC50: 42 nM). LXRα agonist 1 also has a certain agonistic effect on LXRβ (EC50: 266 nM). LXRα agonist 1 promotes target gene transcription by stabilizing the ligand binding domain (LBD) of LXRα. LXRα agonist 1 exhibits potent antitumor effects in hepatocellular carcinoma cells when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the study of lipotoxic cancers .
    LXRα agonist 1
  • HY-403733C
    JJ-450

    		Androgen Receptor Cancer
    JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
    JJ-450
  • HY-164552
    ZNU-IMB-Z15

    		Apoptosis Androgen Receptor Cancer
    ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
    ZNU-IMB-Z15
  • HY-403733B
    (+)-JJ-450

    		Androgen Receptor Prostaglandin Receptor Cancer
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .
    (+)-JJ-450
  • HY-173408
    Nur77 agonist-1

    		Nuclear Hormone Receptor 4A/NR4A Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase Cancer
    Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
    Nur77 agonist-1
  • HY-403733A
    (–)-JJ-450

    		Androgen Receptor Cancer
    (-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
    (–)-JJ-450
  • HY-W017113
    2-Mercaptobenzothiazole

    		Endogenous Metabolite Aryl Hydrocarbon Receptor Metabolic Disease
    2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
    2-Mercaptobenzothiazole

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