Search Result

Results for "

immune-checkpoint

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Checkpoint Kinase (Chk) (2) Apoptosis (2) CCR (1) CD28 (2) CD73 (1) CTLA-4 (3) CXCR (1) Cytochrome P450 (1) DNA Stain (1) E3 Ligase Ligand-Linker Conjugates (1) ERK (1) Eukaryotic Initiation Factor (eIF) (1) IFNAR (1) IKZF Family (1) Interleukin Related (1) LAG-3 (3) Ligands for Target Protein for PROTAC (2) MMP (1) Molecular Glues (1) NOD-like Receptor (NLR) (1) Parasite (1) PD-1/PD-L1 (15) Potassium Channel (1) Prostaglandin Receptor (1) Sodium Channel (1) STAT (1) Target Protein Ligand-Linker Conjugates (2) Transmembrane Glycoprotein (3) VEGFR (1) VISTA (1)
By Research Areas:	Cancer (35) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (22)

By Targets:

Checkpoint Kinase (Chk) (2)

Apoptosis (2)

CCR (1)

CD28 (2)

CD73 (1)

CTLA-4 (3)

CXCR (1)

Cytochrome P450 (1)

DNA Stain (1)

E3 Ligase Ligand-Linker Conjugates (1)

ERK (1)

Eukaryotic Initiation Factor (eIF) (1)

IFNAR (1)

IKZF Family (1)

Interleukin Related (1)

LAG-3 (3)

Ligands for Target Protein for PROTAC (2)

MMP (1)

Molecular Glues (1)

NOD-like Receptor (NLR) (1)

Parasite (1)

PD-1/PD-L1 (15)

Potassium Channel (1)

Prostaglandin Receptor (1)

Sodium Channel (1)

STAT (1)

Target Protein Ligand-Linker Conjugates (2)

Transmembrane Glycoprotein (3)

VEGFR (1)

VISTA (1)

By Research Areas:

Cancer (35)

Cardiovascular Disease (1)

Infection (1)

Inflammation/Immunology (22)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Targets Recommended: Checkpoint Kinase (Chk)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P99617

Fianlimab REGN3767	LAG-3	Inflammation/Immunology Cancer
Fianlimab (REGN3767) is a human monoclonal antibody that targets the immune checkpoint receptor LAG-3 on T cells and has anti-tumour activity .

HY-102011

BMS-1166 3 Publications Verification	PD-1/PD-L1	Inflammation/Immunology Cancer
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC₅₀ of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .

HY-102011A

BMS-1166 hydrochloride 3 Publications Verification	PD-1/PD-L1	Inflammation/Immunology Cancer
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC₅₀ of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .

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 .

HY-150879

BMS-37	PD-1/PD-L1 Ligands for Target Protein for PROTAC	Cancer
BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor. BMS-37 can be used as PD-L1 ligand to synthesize PROTAC molecules .

HY-P99895

Rulonilimab	PD-1/PD-L1	Inflammation/Immunology Cancer
Rulonilimab is a human IgG1 monoclonal antibody against PD-1 that targets, binds and inhibits PD-1 and its downstream signalling pathways with potential immune checkpoint inhibition and anti-tumour activity .

HY-P99698

Lesabelimab LDP	PD-1/PD-L1	Inflammation/Immunology Cancer
Lesabelimab (LDP) is an immunoglobulin G1-kappa anti-CD274 monoclonal antibody. CD274 is an immune checkpoint ligand, represses antitumour immunity through the interaction with PDCD1 receptor .

HY-P990041

Firastotug ADG-116	CTLA-4	Inflammation/Immunology Cancer
Firastotug is an IgG1κ antibody targeting CTLA4. CTLA4 is a cytotoxic T lymphocyte-associated protein and a key immune checkpoint in the fields of autoimmunity and cancer .

HY-162810

ICOS-IN-1	CD28	Others
ICOS-IN-1 (compound 9) is an inhibitor of the interaction between ICOS and ICOS-L (IC₅₀=29.38 μM) and has activity in recognizing immune checkpoints .

HY-151559

Zn-DPA-maytansinoid conjugate 1	Checkpoint Kinase (Chk) STAT CXCR CCR	Cancer
Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .

HY-P990046

Tuparstobart Incagn-02385	LAG-3	Inflammation/Immunology
Tuparstobart (Incagn-02385) is an IgG1κ antibody targeting LAG-3. LAG-3 is an immune checkpoint receptor protein mainly expressed on activated T cells, NK cells, B cells and plasmacytoid dendritic cells .

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-176203

XC-12	CD73	Cancer
XC-12 is an orally active and potent small-molecule CD73 inhibitor (an immune checkpoint) with IC₅₀ values of 12.36 nM and 1.29 nM against soluble and membrane-bound CD73 forms, respectively. XC-12 is promising for research of cancers .

HY-162811

LAG-3 biner 1	LAG-3	Cancer
LAG-3 biner 1 (compound 3) is a small molecule ligand (K_d=1.23 μM) for the immune checkpoint lymphocyte activation gene 3 (LAG-3). LAG-3 biner 1 can be used in the research of cancer diagnosis targeting LAG-3 .

HY-P99378

Neihulizumab ALTB-168; Anti-PSGL1/CD162 Reference Antibody (neihulizumab)	Apoptosis	Inflammation/Immunology
Neihulizumab (ALTB-168) is an immune checkpoint agonistic antibody that binds to human CD162 (PSGL-1), leading to downregulation of activated T-cells. Neihulizumab can be uesd for steroid-refractory acute graft-versus-host-disease (SR-aGVHD), psoriasis, psoriatic arthritis and ulcerative colitis research .

HY-169853

M351-0056	VISTA	Inflammation/Immunology
M351-0056 is the agonist for the immune checkpoint protein VISTA, that reduces the secretion of VISTA-induced cytokines, promotes the T-cell proliferation induced by VISTA, and exhibits immunomodulatory activity. M351-0056 ameliorates Imiquimod (HY-B0180)-induced psoriatic dermatitis in mouse models .

HY-120635

BMS-1001 hydrochloride	PD-1/PD-L1	Inflammation/Immunology Cancer
BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC₅₀ value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .

HY-120647

BMS-1001	PD-1/PD-L1	Inflammation/Immunology Cancer
BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC₅₀ value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .

HY-P9986

Tiragolumab MTIG-7192A; RG-6058	CD28	Cancer
Tiragolumab is an immune checkpoint inhibitor binding to the T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab in combination with Atezolizumab (HY-P9904) and Bevacizumab (HY-P9906) has benefit in unresectable hepatocellular carcinoma. Tiragolumab can be used to study non-small cell lung cancer (NSCLC) and melanoma .

HY-117161

ZINC05626394	Cytochrome P450	Cancer
ZINC05626394 is a cytochrome b5 reductase 3 inhibitor with activity by increasing nitric oxide bioavailability. ZINC05626394 may have potential applications in anti-cancer suppression, especially in combination with antibody drug conjugates (ADCs) and immune checkpoint inhibitors. The efficacy of ZINC05626394 may be limited by different mechanisms, including antigen-related resistance and failure of endocytosis .

HY-P99032

Monalizumab 3 Publications Verification IPH2201	Checkpoint Kinase (Chk) IFNAR	Inflammation/Immunology Cancer
Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC) .

HY-101093

CA-170 1 Publications Verification	PD-1/PD-L1	Inflammation/Immunology Cancer
CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .

HY-P99051

Tinurilimab BAY 1834942	Transmembrane Glycoprotein	Inflammation/Immunology Cancer
Tinurilimab (Bay 1834942) is an anti-CEACAM6 (carcinoembryonic antigen-related cell adhesion molecule 6) humanized IgG2 monoclonal antibody. CEACAM6 is an immune checkpoint regulator suppressing the activity of effector T-cells against tumors. Tinurilimab shows an increased tumor cell killing effect in the tumor-cell/T-cell co-culture system .

HY-W158030

2-Guanidinobezimidazole 2GBI	NOD-like Receptor (NLR)	Cancer
2-Guanidinobezimidazole is a selective agonist of NLRP3, with a K_D 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 .

HY-148305

PD-1/PD-L1-IN-28	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC₅₀=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity .

HY-P990031

Dargistotug M-6223	Transmembrane Glycoprotein	Inflammation/Immunology Cancer
Dargistotug (M-6223) is a fully human IgG1 monoclonal antibody targeting TIGIT (T cell immune receptor with Ig domain and ITIM). TIGIT is an inhibitory immune checkpoint that promotes NK cell depletion and reduces the secretion of cytokines by binding to CD155 and other antibodies. It can also directly or indirectly inhibit effector T cells and upregulate Tregs cells, thereby exerting immunosuppression. Function .

HY-163844

PD-1/PD-L1-IN-49	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 .

HY-13735H

Quinacrine acetate Acriquine acetate	Parasite Sodium Channel DNA Stain Apoptosis	Cancer
Quinacrine (Acriquine) acetate is a small molecule modulator of the cGAS-STING-TBK1 signaling pathway, possessing immune stimulatory activity. Quinacrine acetate has been explored for its potential therapeutic applications in enhancing anti-tumor immunity. Quinacrine acetate can improve the effectiveness of cancer immunotherapies by addressing the poor immunogenicity of various tumors. Quinacrine acetate also presents a promising strategy for overcoming the limitations associated with immune checkpoint inhibitors in cancer treatment.

HY-P990061

Polzastobart JTX 8064	Transmembrane Glycoprotein	Inflammation/Immunology Cancer
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor .

HY-145239

PD-1/PD-L1-IN-13	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC₅₀ value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 ⁺ T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .

HY-145240

eIF4E-IN-1	Eukaryotic Initiation Factor (eIF)	Infection Cancer
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y) .

HY-120646

BMS-242	PD-1/PD-L1	Others
BMS-242 is a small molecule PD-1/PD-L1 inhibitor with the activity of inhibiting the PD-1/PD-L1 interaction. BMS-242 can bind to the hydrophobic channel pocket between PD-L1 molecules, inhibit the PD-1/PD-L1 immune checkpoint pathway, and provide a new way for cancer inhibition.

HY-156649

Vorbipiprant CR6086	Prostaglandin Receptor Interleukin Related MMP PD-1/PD-L1	Cardiovascular Disease Inflammation/Immunology Cancer
Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (K_i: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer .

HY-141431

Cbl-b-IN-2	E3 Ligase Ligand-Linker Conjugates	Inflammation/Immunology Cancer
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .

HY-131386A

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride	Target Protein Ligand-Linker Conjugates	Cancer
BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM .

HY-131386

BMS-1166-N-piperidine-CO-N-piperazine	Target Protein Ligand-Linker Conjugates	Cancer
BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM .

HY-172930

PVTX-405	Molecular Glues IKZF Family Potassium Channel	Inflammation/Immunology Cancer
PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC₅₀ of 0.7 nM and a D_max of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC₅₀ of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn ^391V C57BL/6 mice .

HY-131187

BMS-1166-N-piperidine-COOH	Ligands for Target Protein for PROTAC	Cancer
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1 . BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC₅₀ of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation .

HY-152293

EVT801	VEGFR ERK	Cancer
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC₅₀=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name

HY-L184

Anti-Gastric Cancer Compound Library	871 compounds
Gastric Cancer (GC) is one of the most common malignant tumors in the world, ranking fourth in mortality rate globally. Because the early symptoms of stomach neoplasm are usually not obvious, are diagnosed with gastric cancer at terminal stage, and the relative survival rate within 5 years is very low. With the further understanding of the molecular characteristics of stomach neoplasm, many therapeutic targets for gastric cancer have been identified, and molecular targeted therapies such as CTLA-4, HER2 and immune checkpoint inhibitors have made rapid progress. Although survival rates for patients with gastric neoplasm have improved over the past few decades, the prognosis is still worrying. Therefore, there is an urgent need for new drugs to treat gastric cancer. MCE designs a unique collection of 871 small molecules with definite or potential anti-gastric cancer activity, which is an important tool for studying the pathological mechanism of stomach neoplasm and developing drugs for stomach neoplasm.

Anti-Gastric Cancer Compound Library

871 compounds

Gastric Cancer (GC) is one of the most common malignant tumors in the world, ranking fourth in mortality rate globally. Because the early symptoms of stomach neoplasm are usually not obvious, are diagnosed with gastric cancer at terminal stage, and the relative survival rate within 5 years is very low. With the further understanding of the molecular characteristics of stomach neoplasm, many therapeutic targets for gastric cancer have been identified, and molecular targeted therapies such as CTLA-4, HER2 and immune checkpoint inhibitors have made rapid progress. Although survival rates for patients with gastric neoplasm have improved over the past few decades, the prognosis is still worrying. Therefore, there is an urgent need for new drugs to treat gastric cancer.

MCE designs a unique collection of 871 small molecules with definite or potential anti-gastric cancer activity, which is an important tool for studying the pathological mechanism of stomach neoplasm and developing drugs for stomach neoplasm.

Cat. No.	Product Name	Target	Research Area

HY-P10715

Fmoc-KCRGDK	Peptides	Inflammation/Immunology Cancer
Fmoc-KCRGDK is a self-assembling peptide that can be used to prepare hydrogels and assist in drug delivery for immune checkpoint inhibitors. Fmoc-KCRGDK can be applied in cancer immunotherapy research .

Cat. No.	Product Name	Target	Research Area