programmed cell death

Concanavalin A is a natural product, a phytoalexin (glycan-binding protein). Concanavalin A has antitumor activity and can also induce acute liver injury.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

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.

Phosphorylethanolamine (O-Phosphorylethanolamine) is a phosphomonoester metabolite of the phospholipid metabolism. Phosphorylethanolamine is a precursor of phospholipid synthesis and a product of phospholipid breakdown. Phosphomonoesters are present at much higher levels in the brain than in other organs. In developing the brain, phosphomonoesters are normally elevated during the period of neuritic proliferation. This also coincides with the occurrence of normal programmed cell death and synaptic pruning in developing the brain. These findings are consistent with the role of phosphomonoesters in membrane biosynthesis. Phosphorylethanolamine shows a strong structural similarity to the inhibitory neurotransmitter, GABA, and the GABAB receptor partial agonist, 3-amino-propylphosphonic acid. Phosphorylethanolamine is a phosphomonoester which is decreased in post-mortem Alzheimer's disease (AD) brain.

2-aminobenzo[d]thiazol-6-ol has antimicrobial, antioxidant and anticancer properties and may inhibit the activity of certain cancer cell lines by inducing apoptosis or programmed cell death.

Apoptosis Inhibitor was a novel inhibitor of programmed cell death associate with caspase-3 inhibition.

2-amino-4-methyl-1,3-thiazole-5-carbohydrazide (AMTCH) has antitumor activity and inhibits the growth of cancer cells by inducing apoptosis or programmed cell death. It also has antibacterial and fungal activity.

PD-1-IN-17 TFA is a inhibitor of programmed cell death-1 (PD-1) .

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

Lipid C2 is an ionizable cationic lipid utilized in the formation of lipid nanoparticles (LNP) for the delivery of mRNA in vivo. LNPs containing Lipid C2 and encapsulating mRNA reporter genes specifically accumulate in the liver and spleen of mice, while avoiding the heart, lungs, and kidneys. Additionally, LNPs with Lipid C2 that encapsulate mRNA encoding Epstein-Barr virus (EBV) protein Latent Membrane Protein 2 (LMP-2), when combined with anti-programmed cell death protein 1 (PD-1) antibodies, have been shown to reduce tumor size, reverse T cell exhaustion, increase the percentage of CD3+CD8+ central T cells and CD3+CD8+ effector memory T cells in the spleen, and decrease the percentage of CD3+T cells expressing Pd-1 in a CT26 mouse model of EBV-infected colon cancer.

BG11 promotes the accumulation of Fe2+ and intracellular lipid peroxides, leading to ferroptosis (iron-dependent cell death). It regulates the expression of Bax and Bcl-2 proteins, inducing apoptosis (programmed cell death) in MDA-MB-231 cells. BG11 also causes cell cycle arrest at the G0/G1 and S phases, inhibiting the proliferation of TNBC cancer cells, with IC50 values of 0.49 μM for MDA-MB-231 and 0.52 μM for BT549. Additionally, it reduces cell migration and invasion and demonstrates antitumor effects in mouse models.

Antiparasitic agent-26 (Compound 8) is an antiparasitic compound that effectively inhibits the growth of Naegleria fowleri, with an IC50 of 22.87 μM (trophozoite stage) and 25.16 μM (cyst stage). It exerts its antiparasitic effects by inducing programmed cell death, which includes cytosolic calcium accumulation, mitochondrial membrane potential collapse, ATP synthesis inhibition, ROS accumulation, and chromatin condensation. Antiparasitic agent-26 can be utilized in research on primary amoebic meningoencephalitis (PAM).

TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.

PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.

PLD1 inhibitor is a compound that targets phospholipase D1 (PLD1). It suppresses PLD activity in A549 cells overexpressing PLD1 with an IC50 of 1.97 µM. This inhibitor also decreases the viability of A549 lung cancer and HCT116 colorectal cancer cells, with IC50 values of 18 and 29 µM, respectively. Furthermore, it impairs proliferation, migration, and invasion of A549 cells and triggers apoptosis. Administered at 10 mg/kg every other day, PLD1 inhibitor diminishes tumor growth, induces intratumoral apoptosis, and lowers levels of Ras, CD47, CD24, and programmed cell death 1 ligand 1 (PD-L1) in a murine Lewis lung carcinoma model.

PD-1/PD-L1 antagonist 1 (Compound A5) is an inhibitor of the interaction between programmed cell death protein 1 (PD-1) and programmed death-ligand 1 (PD-L1), with an IC50 value of 23.78 nM.

Antiparasitic agent-27 (Compound 2) is a potent antiparasitic compound targeting Leishmania infantum with an IC50 of 3.1 μM. It induces cell cycle arrest in the G0/G1 phase and enhances reactive oxygen species (ROS) production to trigger programmed cell death, showing promise for visceral leishmaniasis (VL) research.

12-Oxo phytodienoic acid (12-oxo PDA) is an endogenous signal converter that increases alkaloid biosynthesis in E. californica cell cultures, increases b. dioica tendril curls, And inhibited jasmonic acid-induced programmed cell death in conditioned A. fru mutants.

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Kocik, J., et al.Di-bromo-based small-molecule inhibitors of the PD-1/PD-L1 immune checkpointJ. Med. Chem.63(19)11271-11285(2020)

LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).