PD-1/PD-L1 Inhibitor

Anti-PD-L1/B7-H1 Antibody (29E.2A3) is a kind of mouse IgG2b κ chimeric antibody inhibitor, targeting to human PD-L1/B7-H1. Anti-PD-L1/B7-H1 Antibody (29E.2A3) can block the binding of PD-1 to PD-L1. Anti-PD-L1/B7-H1 Antibody (29E.2A3) can be used for the research of infection, such as hepatitis C virus (HCV).

PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC₅₀s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases.

Sec61-IN-2 is a Sec61 inhibitor. Sec61-IN-2 shows a significant inhibitory effect on PD-1 related reporter gene cell models (PD1tsGluc) (IC₅₀ = 42 nM), while it has almost no inhibitory activity in TNFα, Her3, and IL-2 pathway models. Sec61-IN-2 can be used for cancer research.

Prolgolimab (BCD-100) is a human IgG1 anti-PD-1 monoclonal antibody containing the Fc-silencing 'LALA' mutation. Prolgolimab can be used for the research of advanced melanoma.

PD-1-IN-24 (compound 1) is an orally active PD-1 inhibitor.

PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research.

LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC₅₀ of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer.

PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC₅₀ value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity.

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer.

OPBP-1 is a D-peptide obtained by phage display screening, molecular docking and molecular dynamics simulation. OPBP-1 has high stability and strong antitumor and oral activity. OPBP-1 can selectively bind PD-L1 protein, significantly block the interaction between PD-1 and PD-L1, and this blocking effect helps to restore and improve the function of T lymphocytes and reduce the proportion of bone marrow derived suppressor cells (MDSCs) to combat tumor-induced immune escape. OPBP-1 can be used in cancer immunotherapy research.

(Rac)-Chem-0199 is the racemic mixture of Chem-0199 (HY-178193). Chem-0199 is an Adipocyte Enhancer-Binding Protein 1 (AEBP1) inhibitor. Chem-0199 can disrupt the interaction between AEBP1 and CKAP4, thereby enhances antitumor immunity. Chem-0199 can inhibit Akt phosphorylation (p-Akt) and downregulates PD-L1 expression. Chem-0199 can be used for the research of cancer, such as colon cancer.

BMS-200 is a potent PD-1/PD-L1 interaction inhibitor with an IC₅₀ of 80 nM. BMS-200 can induce dimerization of PD-L1.

Nebratamig (GNC-035) is an anti-ROR1/anti-CD3/anti-PD-L1/anti-4-1BB tetra-specific antibody with potential immunostimulatory and antineoplastic activities.

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.

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (K_d=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC₅₀s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo.

PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC₅₀ of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model.

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.

Fidasimtamab is a bispecific antibody targeting human epidermal growth factor receptor 2 (Her2) and programmed death protein 1 (PD-1), with a K_a of 3.55e-10 M for human Her2 and a K_a of 1.17e-9 M for human PD-1. Fidasimtamab cross-links Her2-positive tumor cells with PD-1-positive T cells to form immune synapses, blocks PD-1-ligand interactions, preserves antibody-dependent cellular cytotoxicity, induces gasdermin B (GSDMB)-mediated pyroptosis, and activates T cells. Fidasimtamab is applicable to relevant research on Her2-positive gastric cancer.

Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (K_D = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors.

Rilvegostomig (AZD-2936) is a bispecific humanized IgG1 antibody targeting PD-1 and TIGIT. Rilvegostomig induces tumor growth inhibition and modulates the tumor immune microenvironment. Rilvegostomig exhibits anti-tumor activity in metastatic non-small cell lung cancer (without prior immune checkpoint inhibitor treatment). Rilvegostomig can be used in research related to metastatic non-small cell lung cancer and endometrial cancer.