Tag: p53

NU9056 is a Selective Tip60 (KAT5) Histone Acetyltransferase Inhibitor

Histone acetylation and deacetylation are key events in the regulation of chromatin structure. Additionally, Histone acetyltransferases (HATs) can catalyze acetyl groups to the ε-amino terminus of lysine residues within histones. Acetylation results in an open chromatin structure by removing positive charges from histones. As a result, it induces protein...

MD-222 is a First-in-Class Highly Potent PROTAC Degrader of MDM2

PROTACs are heterobifunctional molecules that connect a POI ligand to an E3 ubiquitin ligase recruiting ligand with an optimal linker. Researchers reported the discovery of MD-222. MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53...

HLI373 is an Efficacious Hdm2 Inhibitor, with Antimalarial Activity

Hdm2 is an ubiquitin-protein ligase. Hdm2 suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. HLI373 is an efficacious Hdm2 inhibitor. HLI373 is effective in inducing apoptosis of several tumor cell lines that are sensitive to DNA-damaging agents. These results suggest that HLI373 could serve...

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...

CG-200745, a HDAC Inhibitor, Induces the Accumulation of p53

Histone deacetylase (HDAC) inhibits are considered to be promising agents that can be used as treatments for cancer. CG-200745 is a novel and potent hydroxamate-based pan-HDAC inhibitor. CG-200745 has the hydroxamic acid moiety to bind zinc at the bottom of the catalytic pocket. We will introduce its anti-tumorigenic property...

PTC596 is an Orally Active and Selective BMI-1 Inhibitor

BMI-1 is a highly conserved class II member of the Polycomb group of genes, regulating diverse aspects of transcription, stem cell maintenance, cell proliferation, and oncogenesis. BMI-1 has vital functions in the self-renewal and maintenance of AML and normal hematopoietic stem cells. The first BMI inhibitor PCT-209 has a...

MD-224 is a First-in-Class and Highly Potent PROTAC Degrader of MDM2

As previously introduced, the tumor suppressor p53 plays a critical role in the prevention of tumor development. While human, murine double minute 2 (MDM2) protein is a primary endogenous cellular inhibitor of the tumor suppressor p53. And it has been pursued as a promising cancer therapeutic target. A study...