SZUH280 is a Potent And Selective PROTAC HDAC8 Degrader
Histone deacetylase 8 (HDAC8) is a class I histone deacetylase. Unlike other class I HDACs, it localizes both in the nucleus and in the cytoplasm. HDAC8 can also target non-histone proteins, such as the structural maintenance of chromosome 3 (SMC3) cohesin protein, retinoic acid induced 1 (RAI1) and p53....
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...
U7D-1 is a Selective USP7 PROTAC Degrader For Leukemia Research
Ubiquitin-specific proteinase 7 (USP7) is a kind of de ubiquitination enzyme (DUB), which can remove ubiquitin and protect substrate protein from degradation. Besides, the full activity of USP7 requires the C-terminal Ub-like domain to fold back to the catalytic domain. Moreover, this allows the active site to be remodeled...
GN25 is a Specific p53-Snail Binding Inhibitor with Antitumor Effects
P53, also known as Tumor protein P53, or transformation-related protein 53 (TRP53) is a regulatory protein that is often mutated in human cancers. Besides, p53 is the strongest tumor suppressor gene. In addition, p53 also induces cell death, and growth arrest and suppresses metastasis in response to various kinds...
CBL0137 is an Histone Chaperone FACT Inhibitor
Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...
MB710 is a Stabilizer of Oncogenic p53 Mutation Y220C
p53 acts as a tumor suppressor protein. Additionally, it plays s a pivotal role in several critical cellular processes, including cell-cycle regulation, DNA repair, and apoptosis. The p53 protein exerts its tumor suppressor function through complex and intricate regulatory processes. The tumor suppressor protein p53 plays a pivotal role...
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...