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Results for "

PD-1 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PD-1/PD-L1 (10) Adenosine Receptor (1) Apoptosis (1) Aryl Hydrocarbon Receptor (3) c-Kit (2) CTLA-4 (1) Discoidin Domain Receptor (2) Dopamine Receptor (2) Drug-Linker Conjugates for ADC (1) Endogenous Metabolite (1) FLT3 (2) iGluR (3) LAG-3 (1) mGluR (1) Monoamine Oxidase (1) Phosphatase (1) Prostaglandin Receptor (1) TNF Receptor (1) Toll-like Receptor (TLR) (2) Trk Receptor (2) VEGFR (2)
By Research Areas:	Cancer (18) Infection (1) Inflammation/Immunology (4) Neurological Disease (10)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Natural
Products

Targets Recommended: PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P99203

Cemiplimab	PD-1/PD-L1	Cancer
Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research .

HY-P99166

Vudalimab	PD-1/PD-L1 CTLA-4	Inflammation/Immunology Cancer
Vudalimab is a potent dual *PD-1* and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .

HY-P99052

Tislelizumab 2 Publications Verification	PD-1/PD-L1	Inflammation/Immunology Cancer
Tislelizumab is a monoclonal antibody that specifically binds to programmed cell death receptor 1 (PD-1), blocking its interaction with programmed death ligand 1 (PD-L1) and programmed death ligand 2 (PD-L2). Tislelizumab can reactivate immune cells such as T lymphocytes and enhance anti-tumor activity. Tislelizumab can be used for the research of a variety of tumors including typical Hodgkin's lymphoma, urothelial carcinoma, non-small cell lung cancer and hepatocellular carcinoma .

HY-P9903

Nivolumab Maximum Cited Publications 20 Publications Verification BMS-936558; ONO-4538; MDX-1106	PD-1/PD-L1	Cancer
Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.

HY-P9902

Pembrolizumab 10+ Cited Publications MK-3475; Lambrolizumab	PD-1/PD-L1	Cancer
Pembrolizumab (MK-3475) is a humanized IgG4 antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.

HY-P99489

Budigalimab ABBV 181; PR 1648817	PD-1/PD-L1	Cancer
Budigalimab (ABBV 181; PR 1648817) is a humanized, recombinant IgG1 monoclonal antibody targeting programmed cell death 1 (PD-1) receptor. Budigalimab has an Fc mutation that reduces the inhibition of Fc receptor interactions and effector factors. Budigalimab can block the binding of PD-1 and PD-L1, which has anti-tumor activity. Budigalimab can be used in the study of solid tumors .

HY-P99387

TSR-033	LAG-3	Cancer
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .

HY-P990067

Evunzekibart ATOR-1017	TNF Receptor	Cancer
Evunzekibart (ATOR-1017) is an Fc-γ receptor conditional 4-1BB agonist and IgG4-type antibody. Evunzekibart can be used as monotherapy or in combination with anti-PD1 to exert anticancer activity.

HY-16961

Sitravatinib 3 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 .

HY-P99957

Zeluvalimab AMG-404	PD-1/PD-L1	Cancer
Zeluvalimab (AMG-404) is a monoclonal antibody targeting the **PD-1 receptor** that can be used for the research of cancer .

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 .

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 .

HY-N12537A

(2R,3S)-PD-1/PD-L1-IN-38	Aryl Hydrocarbon Receptor PD-1/PD-L1	Cancer
(2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8 ⁺T cells and inhibits the signal transduction of PD-1/PD-L1 .

HY-108237

Naxagolide (+)-PHNO; Dopazinol	Dopamine Receptor	Neurological Disease
Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD) .

HY-144497

HE-S2	PD-1/PD-L1 Toll-like Receptor (TLR) Drug-Linker Conjugates for ADC	Infection Cancer
HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the *PD-1/PD-L1* interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity .

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 .

HY-P99963

Sudubrilimab HS636	PD-1/PD-L1	Cancer
Sudubrilimab (HS636) is an Ig G1-kappa monoclonal antibody against PDL1. Sudubrilimab is fused at the C terminus of the heavy chain to a TGF-β1 receptor Ⅱ ectodomain (TGFBR2-ECD), and which can sequester the PD-1/PD-L1 pathway and TGF-β bioactivity in the immunosuppressive tumor microenvironment .

HY-118238

Remeglurant MRZ-8456	mGluR	Neurological Disease
Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC₅₀ of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .

HY-13993

Ro 25-6981 5+ Cited Publications	iGluR	Neurological Disease
Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD) .

HY-13993B

Ro 25-6981 hydrochloride	iGluR	Neurological Disease
Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD) .

HY-13993A

Ro 25-6981 Maleate 5+ Cited Publications	iGluR	Neurological Disease
Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD) .

HY-136220A

AHR antagonist 5 hemimaleate	Aryl Hydrocarbon Receptor	Cancer
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC₅₀ of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) .

HY-148867

UCM-1306 2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl	Dopamine Receptor	Neurological Disease
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD) .

HY-136220

AHR antagonist 5	Aryl Hydrocarbon Receptor	Cancer
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC₅₀ of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 .

HY-120553

B-355252	Apoptosis	Neurological Disease
B355252, a phenoxy thiophene sulfonamide small molecule, is a potent NGF receptor agonist. B355252 potentiates NGF-induced neurite outgrowth. B355252 protects ischemic neurons from neuronal loss by attenuating DNA damage, reducing ROS production and the LDH level, and preventing neuronal apoptosis. B355252 has anti-apoptotic effects in glutamate-induced excitotoxicity, as well as in a murine hippocampal cell line (HT22) model of Parkinson disease (PD) .

HY-147319

RTI-7470-44	Others	Neurological Disease
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant *human trace amine-associated receptor* subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i** value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .

HY-120826

A2AAR/hMAO-B-IN-1	Monoamine Oxidase Adenosine Receptor	Neurological Disease
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC₅₀: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .

HY-113366

Prostaglandin J2 PGJ2	Prostaglandin Receptor Endogenous Metabolite	Neurological Disease
Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent *PGD2 receptor* (DP) agonist with K_i*s of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC₅₀ value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD)* .

Cat. No.	Product Name

HY-L109

Protein-protein Interaction Inhibitor Library	600 compounds
Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs. However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures. With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 600 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Protein-protein Interaction Inhibitor Library

600 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.

However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 600 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Cat. No.	Product Name	Target	Research Area