PD-1/PD-L1 Inhibitor

CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC₅₀ values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research.

LZFPN-90 (LZ90) is a dual NAMPT/PD-L1 targeting compound. LZFPN-90 inhibits PD-1/PD-L1 interaction and NAMPT activity. LZFPN-90 inhibits cell growth in a NAMPT-dependent manner and blocks the cell cycle, subsequently inducing apoptosis. LZFPN-90 exerted target-dependent antitumor activities, affecting metabolic processes and the immune system.

MEDI-0680 (AMP-514) is a human IgG4 monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. MEDI-0680 can be used in Diffuse Large B-Cell Lymphoma (DLBCL) research.

IMM25011 is an Anti-CD274/PD-L1/B7-H1 antibody.

PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC₅₀ of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases.

RC98 is a monoclonal antibody targeting programmed cell death ligand 1 (PD-L1) and acts as a selective PD-L1 inhibitor. RC98 binds specifically to human and cynomolgus monkey PD-L1. RC98 blocks the interaction between PD-L1 and its receptor PD-1 to reverse T-cell inactivation mediated by PD-1/PD-L1 signaling. RC98 enhances the cytotoxic T-lymphocyte-mediated anti-tumor immune response against PD-L1-expressing tumor cells. RC98 can be used for the research of tumor immunity and solid tumors.

PD-1/PD-L1-IN-18 (Compound L31) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-18 blocks PD-1/PD-L1 with the IC₅₀ of 1.054 μM. Antitumor Activity.

YDH-704 is a PAK1/HDAC10 inhibitor, with IC₅₀ values of 0.05 μM and 0.02 μM against human targets, respectively. YDH-704 blocks PAK1-mediated oncogenic signaling pathways, inhibits the proliferation and migration of tumor cells, suppresses the epigenetic regulatory function of HDAC10, downregulates PD-L1 expression, and regulates polyamine metabolism. YDH-704 reduces MDSC/Treg infiltration, enhances the infiltration and activation of CD8⁺ T cells, and inhibits tumor growth and lung metastasis. YDH-704 can be used for research on triple-negative breast 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.

PD-L1-IN-8 is a PD-L1 inhibitor (IC₅₀ = 0.89 nM). PD-L1-IN-8 shows low CYP inhibition and minimal hERG activity. PD-L1-IN-8 can be used for the study of colon 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.

PD-L1/CD-73-IN-1 (compound CC-5) is PD-L1/CD73 inhibitor with IC₅₀ values of 6 nM and 0.773 μM to PD-L1 and CD73, respectively. PD-L1/CD-73-IN-1 inhibits tumor cell growth in vivo and in vitro.

OSE-279 is a high-affinity humanized monoclonal bivalent antibody targeting PD-1, the recommended isotype control is HY-P99003. OSE-279 blocks PD-1 ligand binding, inhibits PDL1-induced SHP1 phosphorylation, restores T cell activation, and promotes reactivation of primary T cell effector functions. OSE-279 binds hFcRn receptor, predicts long half-life, induces CD4 and CD8 T cell proliferation, and promotes interleukin 2 and interferon gamma secretion. OSE-279 can be used for the research of advanced malignancies, colon cancer, hepatocarcinoma, mesothelioma.

PD-1/PD-L1-IN-15 (Compound M17) is a potent inhibitor of PD-1/PD-L1 with an IC₅₀ value of 60.1 nM. PD-1/PD-L1-IN-15 has the potential for the research of tumor immunoresearch.

AMP-224 is a fusion protein targeting PD-L2. AMP-224 specifically binds to PD-1 T cells (chronically stimulated/exhausted T cells). AMP-224 can be used in Colorectal cancer and Solid tumours research.

BAT-1306 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. BAT-1306 can be used in Colorectal cancer and Solid tumours research.

Penpulimab (Anti-PD-1) is an IgG1 backbone anti-PD-1 monoclonal antibody with antitumor activities.

PD-L1-IN-11 is a PD-L1 inhibitor with human PD-L1 IC₅₀ and K_D of 27.82 μM and 49.50 μM, respectively. PD-L1-IN-11 directly binds to PD-L1 via a dimer-locking mechanism, occluding the PD-1 interaction surface to disrupt PD-1/PD-L1 interaction. PD-L1-IN-11 can be used for the research of melanoma, colon carcinoma.

BMS-202 hydrochloride is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC₅₀ of 18 nM and a K_D of 8 μM. BMS-202 hydrochloride binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 hydrochloride has antitumor activity.

PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC₅₀ of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC₅₀=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME.