pd1/pdl1

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

Avelumab, a fully human IgG1 anti-PD-L1 monoclonal antibody, exhibits potential antibody-dependent cell-mediated cytotoxicity.

D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

PD-1-IN-17 is an inhibitor of programmed cell death-1 (PD-1). PD-1-IN-17 inhibits 92% splenocyte proliferation at 100 nM.

PD-1-IN-22 is a potent inhibitor of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction, with an IC50 of 92.3 nM.

ARB-272572 is a potent inhibitor of programmed cell death ligand 1 (PD-L1) signaling that induces PD-L1 homodimer interactions and produces immunostimulatory activity in human primary cells.

BMS-1166-n-piperidine-co-n-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1/PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1/PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

IMMH 010 maleate (YPD-30 maleate) is an orally available programmed cell death ligand 1 inhibitor with potential antitumor activity for the study of neurological disorders and advanced malignant solid tumors.

ARB-272572 hydrochloride is a small molecule PD-L1 inhibitor with an IC50 value of 400 pM for PD-1/PD-L1 HTRF.ARB-272572 hydrochloride inhibits PD-1/PD-L1 cell signaling by inducing homologous interactions with PD-L1 proteins.

PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.

Sulfamethoxypyridazine (CL 13494) is a sulfanilamide antibacterial agent.

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.

BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.

Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.

PD1-PDL1-IN 1 is a potent inhibitor of programmed cell death 1 (PD-1),and used as immune modulator.

LTB is a prodrug formed through the conjugation of the glycolysis inhibitor (Lonidamine) and the PD1/PDL1 blocker (BMS-1) via a thioketal bond. LTB can encapsulate the photosensitizer Chlorin e6 (Ce6), constructing a co-delivery photodynamic nanoplatfform through self-assembly (LTB-6 NPs).

BMS-8 is a novel inhibitor of the PD-1/PD-L1 interaction (IC50: 7.2 μM) by binding directly to PD-L1 and inducing the formation of PD-L1 homodimers.

Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.

Evixapodlin (PD-1/PD-L1-IN 7) is a human PD-1/PD-L1 protein/protein interaction inhibitor (IC50: 0.213).Evixapodlin has anticancer and antiviral activities.

INCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.

PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS