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ligand-binding

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Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13956S

    U 72107-d4

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
    Pioglitazone-d4
  • HY-13956
    Pioglitazone
    Maximum Cited Publications
    25 Publications Verification

    U 72107

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
    Pioglitazone
  • HY-13956B

    U 72107 potassium

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
    Pioglitazone potassium
  • HY-13956C

    (R)-U 72107

    PPAR Neurological Disease
    (R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
    (R)-Pioglitazone
  • HY-13956R

    PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
    Pioglitazone (Standard)
  • HY-N4194

    PPAR Metabolic Disease
    Glabrone is an isoflavone isolated from Glycyrrhiza glabra roots. Glabrone exhibits anti-influenza activity and significant PPAR-γ ligand-binding activity .
    Glabrone
  • HY-136242

    Androgen Receptor Endocrinology Cancer
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy .
    UT-34
  • HY-N11773

    PPAR Metabolic Disease
    Gancaonin L is an isoflavone, that can be isolated from Glycyrrhiza glabra roots. Gancaonin L exhibits significant PPAR-γ ligand-binding activity. Gancaonin L can be used for anti-diabetes and anti-obesity research .
    Gancaonin L
  • HY-108822

    Arcalyst; IL 1 Trap; Interleukin 1 Trap

    Interleukin Related Inflammation/Immunology
    Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .
    Rilonacept
  • HY-13956S1

    Isotope-Labeled Compounds PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
    Pioglitazone-d4 (alkyl)
  • HY-111254

    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-P2264

    Ephrin Receptor Inflammation/Immunology
    KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .
    KYL peptide
  • HY-132205

    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

    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-122742

    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-N2025

    PPAR Glucosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
    Oroxin A
  • HY-117727

    MIN-102; Hydroxypioglitazone

    PPAR Metabolic Disease
    Leriglitazone (MIN-102; Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM,Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
    Leriglitazone
  • HY-117727A

    MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride

    PPAR Metabolic Disease
    Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM,Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
    Leriglitazone hydrochloride
  • HY-156190

    Others Cancer
    NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1
  • HY-160250

    UGT Metabolic Disease
    UGT1A1-IN-1 (compound 2) is a non-competitive inhibitor of UGT1A1, which can inhibit the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. UGT1A1-IN-1 (compound 2) can bind on UGT1A1 at the same ligand-binding site as bilirubin (HY-N0323). UGT1A1-IN-1 can serve as a ‘turn-on’ fluorescent probe substrate for UGT1A1 .
    UGT1A1-IN-1
  • HY-117727S

    MIN-102-d4; Hydroxypioglitazone-d4

    Isotope-Labeled Compounds PPAR Metabolic Disease
    Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM .
    Leriglitazone-d4
  • HY-156190A

    Others Cancer
    NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1 free base
  • HY-111844

    SNIPERs PROTACs RAR/RXR Cancer
    PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
    PROTAC RAR Degrader-1
  • HY-101601

    TAK-427

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
    Bamirastine
  • HY-119782

    Fluorescent Dye Others
    L-Argininamide is a hydrophilic amino acid derivative and can be used as a compound for ligand binding DNA aptamers. L-Argininamide has the potential for fluorescent aptasensors development .
    L-Argininamide
  • HY-D1398

    nAChR Neurological Disease
    LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
    LtIA-F
  • HY-135345

    PROTACs FKBP Cancer
    PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader .
    PROTAC FKBP Degrader-3
  • HY-130714

    PROTACs Cancer
    TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group .
    TD-165
  • HY-128845

    PROTACs Cancer
    PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader .
    PROTAC CRBN Degrader-1
  • HY-120210

    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-23999

    LOX-1 Cardiovascular Disease
    BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .
    BI-0115
  • HY-128839

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader .
    PROTAC ERRα Degrader-2
  • HY-128838

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader .
    PROTAC ERRα Degrader-1
  • HY-109176
    Giredestrant
    3 Publications Verification

    GDC-9545; RG6171

    Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .
    Giredestrant
  • HY-110392

    Estrogen Receptor/ERR Cancer
    CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .
    CMP8
  • HY-P9977
    Amivantamab
    1 Publications Verification

    JNJ-61186372

    EGFR Cancer
    Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .
    Amivantamab
  • HY-135903

    GDC-9545 tartrate; RG6171 tartrate

    Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .
    Giredestrant tartrate
  • HY-111848A

    SNIPERs PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
    PROTAC AR Degrader-4 TFA
  • HY-111848

    SNIPERs PROTACs Androgen Receptor Cancer
    PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
    PROTAC AR Degrader-4
  • HY-B1322A
    Amodiaquine
    5+ Cited Publications

    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-14422
    SR1078
    10+ Cited Publications

    ROR Cancer
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
    SR1078
  • HY-B1322

    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-B1322B
    Amodiaquine dihydrochloride
    5+ Cited Publications

    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-156906

    Others Cancer
    UNC3474 is a small molecule ligand, binding with 53BP1. UNC3474 binds the aromatic methyl-lysine binding cage of 53BP1 TT, with a dissociation constant (Kd) of 1.0 ± 0.3 μM. UNC3474 inhibits the recruitment of 53BP1 to DSBs by stabilizing a pre-existing autoinhibited state of 53BP1 in cells .
    UNC3474
  • HY-B1322AS

    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[1][2][3][4].
    Amodiaquine-d10
  • HY-128838A

    Estrogen Receptor/ERR Others
    (rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .
    (rel)-PROTAC ERRα Degrader-1
  • HY-131188

    PROTACs Bcl-2 Family Cancer
    PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively .
    PROTAC Bcl-xL degrader-1
  • HY-B1322AS1

    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-144705

    Cannabinoid Receptor Neurological Disease
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
    GAT564
  • HY-W677684

    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

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