FA16 is a Specific Ferroptosis Inducer with Metabolic Stability

Ferroptosis is an iron-dependent form of regulatory cell death (RCD). Ferroptosis is an oxidative cell death distinct from apoptosis, driven by intense lipid peroxidation. System Xc–-GSH-GPX4 is the main ferroptosis inhibition pathway. Among them, system System Xc– is a cystine/glutamic acid antitransporter. It is responsible for the introduction of...

OTS193320 is a SUV39H2 Methyltransferase Activity Inhibitor

SUV39H2 is a histone lysine-specific methyltransferase. Specifically, SUV39H2 introduced H3K9me3 to induce transcriptional inhibition. This plays a key role in heterochromatin maintenance, DNA repair, more recently, carcinogenesis. Besides, the genetic ablation of SUV39H1 and SUV39H2 genes leads to severe chromosome instability. For example, abnormally long telomeres are less bound...

Tigatuzumab (CS-1008) is a Humanized Death Receptor 5 (DR5) IgG1 mAb

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL), a member of the TNF superfamily of cytokines, is a type 2 membrane protein expressed in the majority of normal tissues. TRAIL can undergo protease cleavage, resulting in a soluble form able to bind to TRAIL death receptors (DRs). Moreover, TRAIL induces apoptosis...

Xentuzumab is a Monoclonal Antibody That Targets IGF Ligands IGF1 and IGF2

IGF, an insulin-like growth factor, regulates cell growth, proliferation, and survival. The IGF system is made up of IGF1, IGF2, insulin, and corresponding receptors. It transmits abnormal signals to cause a variety of cancers. One that stands out is castration-resistant prostate cancer. IGF can either up-regulate IGF-binding proteins or...

TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP

Apoptosis inhibitor proteins (IAP) represent a group of caspases and negative regulators of cell death. Particularly, the IAP protein family prevents cell death by binding to and inhibiting active caspases and is negatively regulated by IAP-binding proteins. In addition to cell death, IAP also acts as an innate immune...

MMRi62, a Ferroptosis Inducer Targeting MDM2-MDM4

MDM2 and MDM4 have established cancer drug targets. Additionally, they are also inhibitors of p53 activity and are amplified in many cancer types. In particular, the targeting of MDM2–p53 interactions is a novel strategy that is pursued to unleash the antitumor activity of p53. Furthermore,  there needs to cover...