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high-affinity ligand

" in MedChemExpress (MCE) Product Catalog:

120

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19

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13956
    Pioglitazone
    Maximum Cited Publications
    47 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-112210
    Shield-1
    5+ Cited Publications

    Shld1

    		 FKBP Others
    Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .
    Shield-1
  • HY-P1464
    Amylin, amide, rat

    Amylin (rat)

    		 Amylin Receptor Metabolic Disease
    Amylin, amide, rat is a potent and high affinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
    Amylin, amide, rat
  • HY-100583
    (-)-(S)-Equol
    2 Publications Verification

    		 Estrogen Receptor/ERR Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
    (-)-(S)-Equol
  • HY-D1027
    Dansylcadaverine
    10+ Cited Publications

    Monodansyl cadaverine

    		 Autophagy Others
    Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
    Dansylcadaverine
  • HY-B1033
    Metergoline
    2 Publications Verification

    		 5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
    Metergoline
  • HY-145938
    OncoFAP

    		FAP Cancer
    OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
    OncoFAP
  • HY-169182
    AK-068

    		Ligands for Target Protein for PROTAC STAT Cancer
    AK-068 is a high-affinity and selective STAT6 ligand, with a Ki of 6 nM. AK-068 demonstrates at least >150- and >85-fold binding selectivity over STAT5A (Ki >1 μM) and STAT5B (Ki >500 μM) proteins, respectively. AK-068 is a ligand for target protein for PROTAC, can be used for synthesis of PROTACs .
    AK-068
  • HY-W020790
    Sialyl-Lewis X
    1 Publications Verification

    sLeX

    		 Endogenous Metabolite Inflammation/Immunology
    Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability?to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
    Sialyl-Lewis X
  • HY-P99036
    Nesvacumab

    		Tie Cardiovascular Disease Inflammation/Immunology Cancer
    Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2 (Ang2) with high affinity, but shows no binding to Ang1. Nesvacumab can be used in vascular researches .
    Nesvacumab
  • HY-P99189
    Cixutumumab

    IMC-A12; NSC742460

    		 IGF-1R Cancer
    Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
    Cixutumumab
  • HY-174982
    YTHDF2 ligand-1

    		YTHDF Cancer
    YTHDF2 ligand-1 (Compound 23) is a competitive, selective, and high-affinity YTHDF2 ligand with an IC50 of 11 μM and a Kd of 1.3 μM. YTHDF2 ligand-1 competes with m 6A-RNA for binding to YTHDF2. YTHDF2 ligand-1 is applicable for cancer research .
    YTHDF2 ligand-1
  • HY-152231
    BODIPY FL thalidomide

    		Fluorescent Dye Ligands for E3 Ligase Others
    BODIPY FL thalidomide is a high-affinity and selective human cereblon (CRBN)-targeting fluorescent probe with a Kd of 3.6 nM. BODIPY FL thalidomide enables use as a probe in time-resolved fluorescence resonance energy transfer (TR-FRET) binding assays for cereblon ligands. BODIPY FL thalidomide supports development of highly sensitive, selective, stable cereblon TR-FRET binding assays (Ex/Em = 502/510 nm) .
    BODIPY FL thalidomide
  • HY-112429
    HJB97
    2 Publications Verification

    		 Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
    HJB97
  • HY-P99345
    Dostarlimab

    TSR-042; ANB-011; WBP-285

    		 PD-1/PD-L1 Cancer
    Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
    Dostarlimab
  • HY-P2112
    DOTA-NOC

    DOTA-Nal3-octreotide

    		 Radionuclide-Drug Conjugates (RDCs) Somatostatin Receptor Others
    DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging . DOTA-NOC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-NOC
  • HY-N0443
    N-Methylcytisine
    2 Publications Verification

    Caulophylline

    		 nAChR Inflammation/Immunology
    N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .
    N-Methylcytisine
  • HY-122607
    DPA-714

    		Mitochondrial Metabolism TSPO Inflammation/Immunology Cancer
    DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
    DPA-714
  • HY-P1840
    Galanin Receptor Ligand M35

    		Neuropeptide Y Receptor Neurological Disease Endocrinology
    Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
    Galanin Receptor Ligand M35
  • HY-154844
    FAP Ligand 1

    		Biochemical Assay Reagents Cancer
    FAP Ligand 1 (FL), a high-affinity FAP small-molecule ligand, is used to target attached drugs to FAP-expressing fibroblasts and can be used in radiation imaging studies of targeted cancers .
    FAP Ligand 1
  • HY-100982
    (E) -4-Hydroxycrotonic acid

    trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA

    		 GABA Receptor Neurological Disease
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
    (E) -4-Hydroxycrotonic acid
  • HY-P99257
    Bleselumab

    ASKP 1240

    		 TNF Receptor Inflammation/Immunology
    Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection .
    Bleselumab
  • HY-130245
    PCSK9 degrader 1

    		PCSK9 Metabolic Disease
    PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
    PCSK9 degrader 1
  • HY-162553
    GNE7599

    		Ligands for E3 Ligase Cancer
    GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .
    GNE7599
  • HY-D2413
    BODIPY FL VH032

    BODIPY FL PEG4-VH032

    		 Fluorescent Dye Others
    BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
    BODIPY FL VH032
  • HY-100583R
    (-)-(S)-Equol (Standard)

    		Reference Standards Estrogen Receptor/ERR Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    (-)-(S)-Equol (Standard) is the analytical standard of (-)-(S)-Equol. This product is intended for research and analytical applications. (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
    (-)-(S)-Equol (Standard)
  • HY-172563A
    BTR2000 TFA

    		Ligands for E3 Ligase Others
    BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 TFA can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .
    BTR2000 TFA
  • HY-118438
    10-Cl-BBQ

    		Aryl Hydrocarbon Receptor Inflammation/Immunology
    10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations .
    10-Cl-BBQ
  • HY-P1520
    Prolactin Releasing Peptide (1-31), human

    		GnRH Receptor Neurological Disease
    Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
    Prolactin Releasing Peptide (1-31), human
  • HY-P1520A
    Prolactin Releasing Peptide (1-31), human acetate

    		GnRH Receptor Neurological Disease
    Prolactin Releasing Peptide (1-31), human (acetate) is a high affinity GPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
    Prolactin Releasing Peptide (1-31), human acetate
  • HY-168440
    Aurora-A ligand 1

    		Ligands for Target Protein for PROTAC Aurora Kinase CDK Cancer
    Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma .
    Aurora-A ligand 1
  • HY-149933
    AM841

    		Cannabinoid Receptor Neurological Disease
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
    AM841
  • HY-103223
    Phortress

    NSC 710305

    		 Cytochrome P450 Cancer
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
    Phortress
  • HY-136280
    Panamesine

    EMD 57445

    		 Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-173291
    Tau ligand-1

    		Tau Protein Neurological Disease
    Tau ligand-1 (Compound 75) is a ligand for aggregated tau protein that can penetrate the blood-brain barrier . In tissues from patients with Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 exhibits high affinity for aggregated tau protein, with equilibrium dissociation constant (KD) values ranging from 1 to 3.8 nM . Tau ligand-1 can serve as a potential positron emission tomography (PET) tracer and holds promise for application in positron emission tomography imaging studies of tau-related diseases in the central nervous system .
    Tau ligand-1
  • HY-103141
    SB-258585 hydrochloride

    		5-HT Receptor Neurological Disease
    SB-258585 is a high affinity ligand for the 5-HT6 receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT6 receptors. SB-258585 can be used to label recombinant and natural 5-HT6 receptor .
    SB-258585 hydrochloride
  • HY-13956S1
    Pioglitazone-d4 (alkyl)

    		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 .
    Pioglitazone-d4 (alkyl)
  • HY-P5964A
    K1 peptide TFA

    		GABA Receptor Neurological Disease
    K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .
    K1 peptide TFA
  • HY-176502
    FKBP12 ligand-3

    		FKBP Cancer
    FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .
    FKBP12 ligand-3
  • HY-133486
    GABAA receptor agent 1

    		GABA Receptor Neurological Disease
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .
    GABAA receptor agent 1
  • HY-172563
    BTR2000

    		Ligands for E3 Ligase Others
    BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .
    BTR2000
  • HY-P99307
    Namilumab

    AMG-203; Anti-Human CSF2 Recombinant Antibody

    		 c-Fms Inflammation/Immunology
    Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with high affinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis .
    Namilumab
  • HY-115462
    PGN-9856

    		Prostaglandin Receptor Inflammation/Immunology
    PGN-9856 is a selective and high affinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
    PGN-9856
  • HY-100723
    THK-523

    		Amyloid-β Neurological Disease
    THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease .
    THK-523
  • HY-124892A
    Acetylethylcholine mustard hydrochloride

    Acetyl-AF64

    		 Histone Acetyltransferase Neurological Disease
    Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC50) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion .
    Acetylethylcholine mustard hydrochloride
  • HY-152576
    CB2R agonist 1

    		Cannabinoid Receptor Inflammation/Immunology
    CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
    CB2R agonist 1
  • HY-P5964
    K1 peptide

    		GABA Receptor Neurological Disease
    K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .
    K1 peptide
  • HY-174977
    P2Y12R ligand-1

    		P2Y Receptor Neurological Disease
    P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [ 18F] can be used in studies of brain PET imaging .
    P2Y12R ligand-1
  • HY-122612
    SB-258585

    		5-HT Receptor Neurological Disease
    SB-258585 is a selective ligand with high affinity for the 5-HT6 receptor, with a pKi value of 8.53 .
    SB-258585
  • HY-129040
    m-Iodobenzylguanidine
    1 Publications Verification

    MIBG; Iobenguane

    		 Monoamine Transporter Neurological Disease Endocrinology Cancer
    m-Iodobenzylguanidine (Iobenguane) is a ligand with high affinity against norepinephrine transporter (NET). m-Iodobenzylguanidine is used as an imaging agent in the diagnostic imaging and radionuclide studies of neuroendocrine tumors, such as neuroblastoma, pheochromocytoma and carcinoid tumor .
    m-Iodobenzylguanidine

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