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Results for "

Immune checkpoints

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Checkpoint Kinase (Chk) (2) Apoptosis (1) CCR (1) CD28 (1) CTLA-4 (4) CXCR (1) DGK (2) E3 Ligase Ligand-Linker Conjugates (2) ERK (1) Eukaryotic Initiation Factor (eIF) (1) FLT3 (1) HIF/HIF Prolyl-Hydroxylase (1) IFNAR (1) LAG-3 (3) Ligands for Target Protein for PROTAC (2) MAP4K (2) METTL3 (1) Necroptosis (1) PD-1/PD-L1 (13) Prostaglandin Receptor (1) RIP kinase (1) Src (1) STAT (1) TAM Receptor (1) Target Protein Ligand-Linker Conjugates (2) Toll-like Receptor (TLR) (1) VEGFR (1)
By Research Areas:	Cancer (41) Endocrinology (1) Infection (1) Inflammation/Immunology (18)

By Targets:

Checkpoint Kinase (Chk) (2)

Apoptosis (1)

CCR (1)

CD28 (1)

CTLA-4 (4)

CXCR (1)

DGK (2)

E3 Ligase Ligand-Linker Conjugates (2)

ERK (1)

Eukaryotic Initiation Factor (eIF) (1)

FLT3 (1)

HIF/HIF Prolyl-Hydroxylase (1)

IFNAR (1)

LAG-3 (3)

Ligands for Target Protein for PROTAC (2)

MAP4K (2)

METTL3 (1)

Necroptosis (1)

PD-1/PD-L1 (13)

Prostaglandin Receptor (1)

RIP kinase (1)

Src (1)

STAT (1)

TAM Receptor (1)

Target Protein Ligand-Linker Conjugates (2)

Toll-like Receptor (TLR) (1)

VEGFR (1)

By Research Areas:

Cancer (41)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (18)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Natural
Products

Targets Recommended: Immune Checkpoint Checkpoint Kinase (Chk)

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 .

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-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-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-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-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-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-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-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-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-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-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-P99032

Monalizumab 2 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-P99617

Fianlimab REGN3767	LAG-3	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-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-P990041

Firastotug	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-149520

HPK1-IN-39	MAP4K	Cancer
HPK1-IN-39 (Compound 10n) is a selective HPK1 Inhibitor (IC₅₀: 29 nM). HPK1-IN-39 inhibits the phosphorylation of SLP76. HPK1-IN-39 can be used for research of cancer immunotherapy .

HY-P99514

Zalifrelimab AGEN1884	CTLA-4	Cancer
Zalifrelimab (AGEN1884) is a fully human IgG1 monoclonal antibody targeting CTLA-4 (CTLA-4). Zalifrelimab antagonizes the inhibitory checkpoints of immune cell activation regulated by CTLA-4 signaling .

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-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-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-132832

Sirpiglenastat DRP-104	Others	Cancer
Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response .

HY-156649

Vorbipiprant CR6086	Prostaglandin Receptor	Endocrinology
Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases .

HY-156677

STC-15	METTL3	Cancer
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .

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-153435

RIP1 kinase inhibitor 5	RIP kinase Necroptosis	Cancer
RIP1 kinase inhibitor 5 (example 1) is a potent inhibitor of RIP1, which is used as a checkpoint kinase to control tumor immunity . RIP1 kinase inhibitor 5 is similar with SIR1-365 (compound 13), which inhibits necrosis and iron death activity .

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-132288

Pom-8PEG	E3 Ligase Ligand-Linker Conjugates	Cancer
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader .

HY-132150A

HPK1-IN-2 dihydrochloride	MAP4K FLT3 Src	Cancer
HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC₅₀<0.05 µΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 µΜ<IC₅₀<0.5 µΜ) and Flt3 (IC₅₀<0.05 µΜ) kinase activities .

HY-117161

ZINC05626394	Others	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-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 .

HY-120646

BMS-242	Others	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-143305

PD-1/PD-L1-IN-25	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-25 (compound D2) is an inhibitor of PD-1/PD-L1 interaction with an IC₅₀ value of 16.17 nM. PD-1/PD-L1-IN-25 activates the antitumor immunity of T cells efficiently in PBMCs. PD-1/PD-L1-IN-25 can be used for the research of cancer .

HY-149667

BMS-332	DGK	Cancer
BMS-332 is adualDGKα/ζlipid kinase inhibitor, with theIC₅₀of 0.005 (DGKα) and 0.001 μM (DGKζ) .

HY-149666

BMS-496	DGK	Cancer
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC₅₀of 0.09 (DGKα) and 0.006 μM (DGKζ) .

HY-N12041

Axl-IN-16	TAM Receptor HIF/HIF Prolyl-Hydroxylase	Cancer
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .

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-155675

TPPC	Others	Cancer
TPPC, a porphyrin cholesterol conjugate, can render cancer cells more sensitive to ICIs. TPPC can enhance photodynamic immunotherapy toward lung cancer .

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-L031

Small Molecule Immuno-Oncology Compound Library	535 compounds
Immuno-Oncology is a type of immunotherapy that has the specific purpose of treating cancer. It works by stimulating our immune system to fight back. Normally, our immune system is able to destroy cancer cells in our body, however sometimes cancer cells can adapt and mutate, effectively hiding from our immune system. This is when tumors can develop and become a threat to our health. Immuno-oncology involves mobilizing lymphocytes to recognize and eliminate cancer cells using the body’s immune system. There are several immuno-oncology treatments available, including Immune cell therapy (CAR-T), monoclonal antibodies (mABs) and checkpoint inhibitors, cytokines and cancer vaccines. MCE Small Molecule Immuno-Oncology Compound Library offers 535 bioactive tumor immunology compounds that target some important checkpoints such as PD1/PD-L1, CXCR, Sting, IDO, TLR, etc. This library is a useful tool for Immuno-oncology research.

Small Molecule Immuno-Oncology Compound Library

535 compounds

Immuno-Oncology is a type of immunotherapy that has the specific purpose of treating cancer. It works by stimulating our immune system to fight back. Normally, our immune system is able to destroy cancer cells in our body, however sometimes cancer cells can adapt and mutate, effectively hiding from our immune system. This is when tumors can develop and become a threat to our health. Immuno-oncology involves mobilizing lymphocytes to recognize and eliminate cancer cells using the body’s immune system. There are several immuno-oncology treatments available, including Immune cell therapy (CAR-T), monoclonal antibodies (mABs) and checkpoint inhibitors, cytokines and cancer vaccines.

MCE Small Molecule Immuno-Oncology Compound Library offers 535 bioactive tumor immunology compounds that target some important checkpoints such as PD1/PD-L1, CXCR, Sting, IDO, TLR, etc. This library is a useful tool for Immuno-oncology research.

HY-L184

Anti-Gastric Cancer Compound Library	687 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 687 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

687 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 687 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-P99698

Lesabelimab LDP	Inhibitory Antibodies	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-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-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-P99051

Tinurilimab BAY 1834942	Inhibitory Antibodies	Inflammation/Immunology Cancer
Tinurilimab (Bay 1834942) is an anti-CEACAM6 monoclonal antibody. CEACAM6 is an immune checkpoint regulator suppressing the activity of effector T-cells against tumors .

HY-P9986

Tiragolumab MTIG-7192A; RG-6058	Inhibitory Antibodies	Inflammation/Immunology Cancer
Tiragolumab is an immune checkpoint inhibitor binding to T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab, alone or in combination with the PD-L1 inhibitor Atezolizumab (HY-P9904), may be effective against multiple solid malignancies-most notably non-small cell lung cancer (NSCLC) .

HY-P990061

Polzastobart JTX 8064	Inhibitory Antibodies	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 .