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...
HM43239 is an Orally Active and Selective FLT3 Inhibitor
Acute myeloid leukemia (AML) is the most common acute leukemia in adults, with an incidence of over 20 000 cases per year in the United States alone. Large chromosomal translocations, as well as mutations in the genes involved in hematopoietic proliferation and differentiation, result in the accumulation of poorly...
Z-VAD-FMK is a Well-Known pan Caspase Inhibitor
Caspase is a family of cysteine proteases that play essential roles in apoptosis (programmed cell death), necrosis, and inflammation. They are named caspases due to their specific cysteine protease activity-a cysteine in its active site nucleophilically attacks and cleaves a target protein only after an aspartic acid residue. There...
ML132 is a Potent and Selective Caspase 1 Inhibitor
Caspases are cysteine proteases with strict specificity for cleaving peptide sequences C-terminal to aspartic acid residues. A prominent member of the pro-inflammatory class is caspase 1. It is responsible for the proteolytic activation of interleukin (IL)-1β and IL-18. IL-1β and IL-18 are cytokines. They play a major role in...
BETd-260 is a Potent PROTAC BET Degrader
The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...
DT2216 is a Selective PROTAC Degrader of BCL-XL
BCL-XL is a member of the Bcl-2 protein family and a transmembrane molecule in mitochondria. Specifically, it acts as an anti-apoptotic protein by blocking the release of mitochondrial contents such as cytochrome c. Besides, BCL-XL is a well-validated cancer target and eventually leads to caspase activation and eventually programmed...
PU02 is an Allosteric Antagonist of 5-HT3 Receptor
Cancer is a usual disease and a leading cause of death in the world. Therefore, developing new agents specifically targeting cancer cells has achieved more and more researches. As it is widely believed that cancer can be treated by inducing tumor cells to undergo senescence or apoptosis, screening for...