Tag: Caspase

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...

Z-LEHD-FMK is a Selective and Irreversible Inhibitor of Caspase-9

TRAIL is a potent inducer of apoptosis of transformed and cancer cells but not of most normal cells. TRAIL induces apoptotic death on binding to either of two proapoptotic TRAIL receptors, TRAIL R1 or TRAIL R2. Moreover, normal cells may resistant to TRAIL because of expressing higher levels of...

SC-43 is a Potent and Orally Active SHP-1 Agonist and STAT3 Phosphorylation Inhibitor

Cholangiocarcinoma (CCA) is the second most common hepatic malignancy after hepatocellular carcinoma (HCC). CCAs are epithelial malignancies that arise from cholangiocytes and are aggressive behavior and advanced clinical stage. STAT3 belongs to a family of transcription factors that relay cytokine receptor-generated signals into the nucleus. STAT3 is activated by...

TAI-1 is an Orally Active and Highly Potent Hec1 Inhibitor

Hec1 (Ndc80) is one of the outer kinetochore proteins and forms heterotetramers with proteins NUF2, SPC25, and SPC24. Specifically, drugs that interfere with mitosis are part of the most successful chemotherapeutic compounds for cancer in clinical practice. Hec1, a component of mitochondria, is overexpressed in a variety of human...

TH1834 is a Specific Tip60 Histone Acetyltransferase (HAT) Inhibitor

Many aspects of genome regulation and metabolism require histone acetylation. Accordingly, dysfunctional histone acetylation has been implicated in numerous diseases, including cancer. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) regulate acetylation of histones and non-histone. HATs catalyze the acetylation of core histones through the addition of an acetyl group...