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blockade

" in MedChemExpress (MCE) Product Catalog:

74

Inhibitors & Agonists

6

Peptides

4

Inhibitory Antibodies

3

Natural
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2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99540

    PSB-205; QL1706 (iparomlimab/tuvonralimab); PBS105

    PD-1/PD-L1 CTLA-4 Cancer
    Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab .
    Tuvonralimab
  • HY-W158030

    2GBI

    NOD-like Receptor (NLR) Cancer
    2-Guanidinobezimidazole is a selective agonist of NLRP3, with a KD value of 1.29 μM to His-GFP-NLRP3. 2-Guanidinobezimidazole binds directly to the LRR domain of NLRP3, promoting inflammasome assembly and activation. 2-Guanidinobezimidazole promotes anti-tumor immunity, inhibits tumor growth, and overcome immune checkpoint blockade (ICB) resistance .
    2-Guanidinobezimidazole
  • HY-B0292A
    Atracurium besylate
    1 Publications Verification

    BW-33A

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
    Atracurium besylate
  • HY-144501

    Toll-like Receptor (TLR) PD-1/PD-L1 Inflammation/Immunology Cancer
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 .
    D18
  • HY-153544

    Toll-like Receptor (TLR) Cancer
    TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy .
    TLR7/8 agonist 9
  • HY-124047

    Cholinesterase (ChE) Neurological Disease
    RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue .
    RX 67668
  • HY-B0292

    BW-33A free acid

    nAChR Cardiovascular Disease Inflammation/Immunology Cancer
    tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation .
    Atracurium
  • HY-B0292AR

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Atracurium (besylate) (Standard) is the analytical standard of Atracurium (besylate). This product is intended for research and analytical applications. Atracurium (BW-33A) besylate is a potent, competitive and non-depolarizing neuromuscular blocking agent. Atracurium besylate also is an AChR receptor antagonist. Atracurium besylate induces bronchoconstriction and neuromuscular blockade. Atracurium besylate promotes astroglial differentiation .
    Atracurium (besylate) (Standard)
  • HY-163844

    PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1, with the IC50 of 77 nM. PD-1/PD-L1-IN-49 activates Jurkat T cells, reflecting successful blockade of the PD-1/PD-L1 immune checkpoint .
    PD-1/PD-L1-IN-49
  • HY-135004

    Adrenergic Receptor Endocrinology
    Su-4029 is an agent that interacts with alpha receptors. It negates the blockade of norepinephrine by the reversible adrenergic blocker phentolamine but not by the irreversible blocker Dibenamine, suggesting Su-4029 acts at the same site as these blockers. Su-4029 pretreatment results in three categories of responses to pressor phenylalkylamines: irreversible blockade of amines with no or only p-hydroxylation, reversible blockade of amines with beta-carbon hydroxylation, and no blockade or augmentation of amines with m and p-hydroxylation or m or p plus beta-hydroxylation. Su-4029 may deform the alpha receptor site affected by adrenergic blocking agents .
    SU-4029 dihydrochloride
  • HY-129254

    Adrenergic Receptor Metabolic Disease
    5-Hydroxy propranolol is a metabolite of Propranolol that can be used to study β-adrenergic receptor blockade .
    5-Hydroxy propranolol
  • HY-121276
    Benperidol
    1 Publications Verification

    Dopamine Receptor Neurological Disease
    Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
    Benperidol
  • HY-116738

    Others Neurological Disease
    Trimecaine, a local neural blockade agent, has a strong depressant effect on the cerebral cortex and the ascending reticular formation of the brain stem .
    Trimecaine
  • HY-101809A

    iGluR Cardiovascular Disease
    CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
    CNS 5161
  • HY-101809

    CNS 5161A

    iGluR Cardiovascular Disease
    CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
    CNS-5161 hydrochloride
  • HY-P0142

    PKG Cardiovascular Disease
    DT-3 is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
    DT-3
  • HY-108594

    Potassium Channel Metabolic Disease
    PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
    PD-118057
  • HY-P0142A

    PKG Cardiovascular Disease
    DT-3 acetate is a membrane-permeable protein kinase G Iα (PKG Iα) inhibitory peptide and shows pharmacological blockade of the cGMP-PKG signalling .
    DT-3 acetate
  • HY-107728

    Neuropeptide Y Receptor Metabolic Disease
    S 25585 is a potent and selective neuropeptide Y (NPY) Y5 receptor antagonist. S 25585 reduces food intake but not through blockade of the NPY Y5 receptor .
    S 25585
  • HY-107697

    iGluR Neurological Disease
    N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity .
    N20C hydrochloride
  • HY-152156

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
    Tubulin inhibitor 11
  • HY-105084A

    Sodium Channel Neurological Disease
    Lubeluzole (dihydrochloride) is a neuroprotective agent which blockades neuronal voltage-gated sodium channels. Lubeluzole (dihydrochloride) also produces both tonic and block of cardiac sodium channels. Lubeluzole (dihydrochloride) is promising for research of antiarrhythmic agents .
    Lubeluzole dihydrochloride
  • HY-141549

    Others Inflammation/Immunology
    BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3 .
    BPK-21
  • HY-126635

    Dopamine Receptor Adrenergic Receptor Others
    Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
    Mafoprazine
  • HY-121276R

    Dopamine Receptor Neurological Disease
    Benperidol (Standard) is the analytical standard of Benperidol. This product is intended for research and analytical applications. Benperidol is a relatively old antipsychotic agent. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade .
    Benperidol (Standard)
  • HY-14408

    Adenosine Receptor Neurological Disease
    Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .
    Lu AA47070
  • HY-155847

    Phosphatase Cancer
    LYP-IN-3 (compound D34) is a selective inhibitor of Lymphoid-tyrosine phosphatase (LYP) (Ki=0.93 μM), and regulates T-cell receptor (TCR) signaling pathway in tumor progress. LYP-IN-3 activates T-cell and inhibits M2 macrophage polarization, but upregulates PD-1/PD-L1 expression. LYP-IN-3 can be leveraged with PD-1/PD-L1 inhibitor, for futher cancer immunotherapy .
    LYP-IN-3
  • HY-N2412

    Chloride Channel Neurological Disease Cancer
    Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade (IC50=9.8 μM) .
    Irisolidone
  • HY-B0423
    Neostigmine Bromide
    1 Publications Verification

    Eustigmin bromide; Neoserine bromide

    Cholinesterase (ChE) Neurological Disease
    Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
    Neostigmine Bromide
  • HY-14828

    SMP-986

    mAChR Metabolic Disease
    Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB) .
    Afacifenacin
  • HY-172348

    Antibiotic Infection
    BRD-9327 is an inhibitor of EfpA. BRD-9327 binds in the outer vestibule without complete blockade of the substrate path to the outside, suggesting its possible inhibition of the movement necessary for alternate access of the transporter. BRD-9327 can be used for anti-tuberculosis study .
    BRD-9327
  • HY-N6636
    Valencene
    1 Publications Verification

    NF-κB Inflammation/Immunology
    Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
    Valencene
  • HY-106305A

    CI 958 trihydrochloride

    DNA/RNA Synthesis Cancer
    Ledoxantrone (CI 958) trihydrochloride is a DNA helicases inhibitor with an IC50 of 0.17 μM. Ledoxantrone trihydrochloride can be used in the study of prostate cancer .
    Ledoxantrone trihydrochloride
  • HY-126635R

    Adrenergic Receptor Dopamine Receptor Others
    Mafoprazine (Standard) is the analytical standard of Mafoprazine. This product is intended for research and analytical applications. Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
    Mafoprazine (Standard)
  • HY-119385

    Dopamine Receptor Neurological Disease
    Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
    Savoxepin mesylate
  • HY-105925

    MCN 2378

    Adrenergic Receptor Cardiovascular Disease
    Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
    Mefenidil
  • HY-B0284A

    Sodium Channel Cardiovascular Disease
    Nifedipine hydrochloride is a potent vasodilator with calcium antagonist activity. Nifedipine hydrochloride is a useful antianginal compound that can also lower blood pressure. Nifedipine hydrochloride exhibits comparable antihypertensive properties to some new compounds, especially in calcium channel blockade. Nifedipine hydrochloride is used in biological activity studies to develop new antihypertensive and/or antianginal compounds .
    Nifedipine hydrochloride
  • HY-P4042

    hepatitis B peptide 4980

    HBV Infection Inflammation/Immunology
    Hepatitis B Virus Receptor Binding Fragment (hepatitis B peptide 4980) is a synthetic peptide analog which specifically binds to Hep G2 cells. Hepatitis B Virus Receptor Binding Fragment is a promising immunogen expected to elicit protective antibodies based on the concept of the attachment blockade pathway of virus neutralization .
    Hepatitis B Virus Receptor Binding Fragment
  • HY-131340

    Phosphodiesterase (PDE) Inflammation/Immunology
    LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
    LASSBio-1632
  • HY-122664

    BRK Cancer
    XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
    XMU-MP-2
  • HY-129492
    GNF4877
    1 Publications Verification

    DYRK GSK-3 Metabolic Disease
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells) .
    GNF4877
  • HY-N6636R

    NF-κB Inflammation/Immunology
    Valencene (Standard) is the analytical standard of Valencene. This product is intended for research and analytical applications. Valencene is a sesquiterpene isolated from Cyperus rotundus, possesses antiallergic, antimelanogenesis, anti-infammatory, and antioxidant activitivies. Valencene inhibits the exaggerated expression of Th2 chemokines and proinflammatory chemokines through blockade of the NF-κB pathway. Valencene is used to flavor foods and drinks .
    Valencene (Standard)
  • HY-P99406

    MCLA 158

    EGFR Cancer
    Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC) .
    Petosemtamab
  • HY-117223

    Potassium Channel Neurological Disease
    GEA 857 is a structural analog of the Serotonin (HY-B1473A) uptake blocker Alaproclate (HY-164011). GEA 857 enhances responses induced by muscarinic receptor agonists by inhibiting certain calcium-dependent potassium channels on membranes, a blockade that can enhance or prolong the muscarinic cholinergic effects. GEA 857 can be used in research on neurodegenerative diseases .
    GEA 857
  • HY-P9902A
    Pembrolizumab (anti-PD-1)
    2 Publications Verification

    MK-3475 (anti-PD-1); Lambrolizumab (anti-PD-1)

    PD-1/PD-L1 Cancer
    Pembrolizumab (anti-PD-1) is a humanized IgG4 antibody and PD-1 inhibitor. Pembrolizumab produces PD-1 blockade, preventing PD-L1 and PD-L2 from connecting to PD-1. This avoids the uncontrolled regulation of T cells on cells that normally express PD-1 .
    Pembrolizumab (anti-PD-1)
  • HY-W424918

    Dopamine Receptor Neurological Disease
    Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.
    Opromazine hydrochloride
  • HY-122140

    Cholinesterase (ChE) Neurological Disease
    ACG548B (compound 24) is a potent inhibitor of acetyl- and butyrylcholinesterase (AChE and BChE) with IC50s of 1.78 and 0.496 μM, respectively. ACG548B has higher AChE affinity and selectivity over BChE and ChoK (choline kinase) .
    ACG548B
  • HY-13954
    A 839977
    1 Publications Verification

    P2X Receptor Neurological Disease Inflammation/Immunology
    A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
    A 839977
  • HY-121037

    EGM1

    Phosphodiesterase (PDE) Cancer
    Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
    Eggmanone
  • HY-P5487

    iGluR Others
    GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
    GluR23Y

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