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Results for "

blockade

" in MedChemExpress (MCE) Product Catalog:

46

Inhibitors & Agonists

6

Peptides

4

Inhibitory Antibodies

3

Natural
Products

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

    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-B0292A
    Atracurium besylate

    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
    D18

    		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
    TLR7/8 agonist 9

    		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
    RX 67668

    		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-121276
    Benperidol

    		Others 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-101809
    CNS-5161 hydrochloride

    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-101809A
    CNS 5161

    		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-108594
    PD-118057

    		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-107728
    S 25585

    		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-P99302
    Lulizumab

    Humanized Anti-CD28 Recombinant Antibody

    		 CD28 Inflammation/Immunology
    Lulizumab (Humanized Anti-CD28 Recombinant Antibody) is a selective CD28 blockade, Lulizumab prevents T cell activation by selectively targeting CD28 signaling .
    Lulizumab
  • HY-152156
    Tubulin inhibitor 11

    		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-107697
    N20C hydrochloride

    		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-141549
    BPK-21

    		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-P0142
    DT-3

    		Guanylate Cyclase Inflammation/Immunology
    DT-3 is a membrane-permeable protein kinase G Iα inhibitory peptide. DT-3 is a guanylyl cyclase? inhibitor and shows pharmacological blockade of the cGMP–PKG signalling .
    DT-3
  • HY-14408
    Lu AA47070

    		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-121276R
    Benperidol (Standard)

    		Others 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-155847
    LYP-IN-3

    		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
    Irisolidone

    		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-B0292
    Atracurium

    BW-33A free acid
    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-14828
    Afacifenacin

    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-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-P4042
    Hepatitis B Virus Receptor Binding Fragment

    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-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-131340
    LASSBio-1632

    		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-P99406
    Petosemtamab

    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-N6636R
    Valencene (Standard)

    		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-P9902A
    Pembrolizumab (anti-PD-1)
    2 Publications Verification

    		 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-122140
    ACG548B

    		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
    Eggmanone

    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-132246
    WWL123 analogue-1

    		MAGL Neurological Disease
    WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
    WWL123 analogue-1
  • HY-150587
    Anti-inflammatory agent 31

    		ERK NF-κB Inflammation/Immunology
    Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver .
    Anti-inflammatory agent 31
  • HY-153543
    TLR7/8 agonist 8

    		Toll-like Receptor (TLR) Cancer
    TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC50s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade .
    TLR7/8 agonist 8
  • HY-13650
    Indisulam
    5 Publications Verification

    E 7070

    		 Molecular Glues Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
    Indisulam
  • HY-103094
    LY266097 hydrochloride

    		5-HT Receptor Inflammation/Immunology
    LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
    LY266097 hydrochloride
  • HY-136310
    PIP4K-IN-a131
    1 Publications Verification

    		 Others Cancer
    PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways .
    PIP4K-IN-a131
  • HY-B0653A
    Levobupivacaine hydrochloride
    2 Publications Verification

    (S)-(-)-Bupivacaine monohydrochloride

    		 Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
    Levobupivacaine hydrochloride
  • HY-16961
    Sitravatinib
    1 Publications Verification

    MGCD516; MG-516

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib malate
  • HY-B0653
    Levobupivacaine

    (S)-(-)-Bupivacaine

    		 Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
    Levobupivacaine
  • HY-155175
    TIM-3-IN-2

    		Tim3 Cancer
    TIM-3-IN-2 (Compound A-41) is a Tim3 inhibitor (KD: 0.61 μM). TIM-3-IN-2 blocks TIM-3 interactions with PtdSer, CEACAM1, and Gal-9. TIM-3-IN-2 inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 reverses the TIM-3-mediated blockade of the production of proinflammatory cytokines, and maximizes the T-cell antitumor activity against AML cell lines .
    TIM-3-IN-2
  • HY-128679
    TBK1/IKKε-IN-5

    		IKK Cancer
    TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
    TBK1/IKKε-IN-5
  • HY-P2265
    SAH-SOS1A

    		Ras Cancer
    SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A
  • HY-P2265A
    SAH-SOS1A TFA

    		Ras Cancer
    SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A TFA
  • HY-153346
    RMC-6291

    		Ras ERK Apoptosis Cancer
    RMC-6291 is an orally active and covalent inhibitor of KRAS G12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
    RMC-6291

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