Search Result

Results for "

PD-1 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PD-1/PD-L1 (13) Adenosine Receptor (1) Apoptosis (1) Aryl Hydrocarbon Receptor (3) c-Kit (2) CMV (1) CTLA-4 (1) Discoidin Domain Receptor (2) Dopamine Receptor (3) Drug-Linker Conjugates for ADC (1) Endogenous Metabolite (1) FLT3 (2) iGluR (3) Interleukin Related (1) mGluR (2) Monoamine Oxidase (1) Phosphatase (1) Prostaglandin Receptor (2) TAM Receptor (2) TNF Receptor (2) Toll-like Receptor (TLR) (2) Trk Receptor (2) VEGFR (2)
By Research Areas:	Cancer (24) Infection (2) Inflammation/Immunology (8) Neurological Disease (12)

By Targets:

PD-1/PD-L1 (13)

Adenosine Receptor (1)

Apoptosis (1)

Aryl Hydrocarbon Receptor (3)

c-Kit (2)

CMV (1)

CTLA-4 (1)

Discoidin Domain Receptor (2)

Dopamine Receptor (3)

Drug-Linker Conjugates for ADC (1)

Endogenous Metabolite (1)

FLT3 (2)

iGluR (3)

Interleukin Related (1)

mGluR (2)

Monoamine Oxidase (1)

Phosphatase (1)

Prostaglandin Receptor (2)

TAM Receptor (2)

TNF Receptor (2)

Toll-like Receptor (TLR) (2)

Trk Receptor (2)

VEGFR (2)

By Research Areas:

Cancer (24)

Infection (2)

Inflammation/Immunology (8)

Neurological Disease (12)

Inhibitors & Agonists

Screening Libraries

Peptides

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 3 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-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-P9903

Nivolumab Maximum Cited Publications 22 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 Maximum Cited Publications 22 Publications Verification 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	Inflammation/Immunology 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-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-W400801

Denfivontinib hydrochloride G-749 hydrochloride	TAM Receptor	Cancer
Denfivontinib (G-749) hydrochloride is an AXL inhibitor that has synergistic antitumor effects with the PD-1 inhibitor Pembrolizumab (HY-P9902). Denfivontinib can enhance the NOD-like receptor pathway, thereby promoting the formation of the NLRP3 inflammasome .

HY-P991529

AGEN-2373	TNF Receptor	Inflammation/Immunology Cancer
AGEN-2373 is a conditionally active agonist antibody targeting the co-stimulatory receptor CD137. GEN-2373 binds to CD137 without disruption of ligand binding. AGEN-2373 stimulates CD137 under receptor clustering conditions. AGEN-2373 can enhance T cell activity when combined with other checkpoint modulators (e.g. PD-1 antagonist and OX40 agonist). AGEN-2373 can be studied in research for human malignancies .

HY-12964

SGI-7079 3 Publications Verification	TAM Receptor	Cancer
SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].

HY-16961

Sitravatinib 5+ Cited Publications 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-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-P5005

VIPhyb	CMV PD-1/PD-L1	Infection Inflammation/Immunology Cancer
VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist. VIPhyb can inhibit VIP signaling, increase T-cell immunity and downregulate *PD1*. VIPhyb can inhibit cancer cell proliferation. VIPhyb can reduce inflammatory cytokine expression. VIPhyb can enhance viral clearance. VIPhyb can be used for the researches of cancer, infection and inflammation and immunology, such as non-small cell lung cancer (NSCLC), cytomegalovirus infection and colitis .

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-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-P990172

Anti-Mouse PD-L1/B7-H1 (D265A) Antibody (10F.9G2)	PD-1/PD-L1	Cancer
Anti-Mouse PD-L1/B7-H1 (D265A) Antibody (10F.9G2) is a recombinant chimeric version of the original 10F.9G2 antibody (HY-P99145). The variable domain sequences are identical to the original 10F.9G2 but the constant region sequences have been switched from rat IgG2b to mouse IgG1. Anti-Mouse PD-L1/B7-H1 (D265A) Antibody (10F.9G2) contains a D265A mutation in the Fc fragment rendering it unable to bind to endogenous Fcγ receptors. Anti-Mouse PD-L1/B7-H1 (D265A) Antibody (10F.9G2) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 (D265A) Antibody (10F.9G2) can be used for the research of cancer.

HY-P990171

Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2)	PD-1/PD-L1	Cancer
Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) is a recombinant chimeric version of the original 10F.9G2 antibody (HY-P99145). The variable domain sequences are identical to the original 10F.9G2 but the constant region sequences have been switched from rat IgG2b to mouse IgG2a. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) contains a LALA-PG mutation in the Fc fragment rendering it unable to bind to endogenous Fcγ receptors. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) can be used for the research of cancer.

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-108237R

Naxagolide (Standard)	Dopamine Receptor	Neurological Disease
Naxagolide (Standard) is the analytical standard of Naxagolide. This product is intended for research and analytical applications. Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD) .

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-107505

CBiPES hydrochloride	mGluR	Neurological Disease
CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC₅₀: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease, such as 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-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-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-169859

EP4 receptor antagonist 7	Prostaglandin Receptor Interleukin Related	Inflammation/Immunology Cancer
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC₅₀ value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC₅₀ value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD ⁸⁺ T cells into tumors in a CT26 murine colon cancer model .

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-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-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	686 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 686 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

686 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 686 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