Category: Cancer

Trichostatin A (TSA) is a Specific Inhibitor of HDAC Class I/II

Histone deacetylases (HDACs) are enzymes that remove acetyl groups from histone and non-histone proteins. To date, 18 different mammalian HDACs have been identified and divided into four classes: the Class I Rpd3-like proteins (HDAC1, HDAC2, HDAC3, and HDAC8); the Class II Hda1-like proteins (HDAC4, HDAC5, HDAC6, HDAC7, HDAC9, and...

Staurosporine is an ATP-competitive Inhibitor of Protein Kinases

Protein kinases are enzymes that catalyze protein phosphorylation. Obviously, Protein kinases include many types of kinases, such as  PKC,PKA, c-Fgr and phosphorylase kinase. Thereinto, PKC, PKA and phosphorylase kinase belong to serine or threonine kinases and c-Fgr belongs to Tyr kinases. Interestingly, diacylglycerol (DG) can activate PKC and the...

Rapamycin is a Specific mTOR Inhibitor

mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. In addition, mTOR links with other proteins and serves as a core...

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...

IV-361 is an Orally Active and Selective CDK7 Inhibitor

Cyclin-dependent kinase 7 (CDK7) is a catalytic subunit of CDK activated kinase (CAK). CAK is a kinase complex that catalyzes T-ring phosphorylation and activates a variety of cyclin-related kinases, including CDK1, CDK2, CDK4, and CDK6. Importantly, CDK7 plays a role at the direct interface between important processes of cell...

E67-2 is a Selective KIAA1718 Jumonji Domain Inhibitor with Low Toxicity

KIAA1718 is a histone demethylase for repressive methyl marks. what’s more, KIAA1718 involves in transcriptional activation. Specifically, KIAA1718, as a PHF2/PHF8 subfamily member, possesses histone demethylase activity specific for histone H3 lysine 9 (H3K9) and histone H3 lysine 9 (H3K27), transcriptionally repressive histone marks. Furthermore, KIAA1718 forms complexes with...

NRX-2663 is an Enhancer of the Interaction between β-Catenin and E3 Ligase

Protein-protein interactions (PPIs) play a key role in nearly every biological function. And PPIs are a promising new class of biological targets for therapeutic intervention. In addition, PPIs governing the recognition of substrates by E3 ubiquitin ligases are critical to cellular function. Using PPI enhancer molecules as a “molecular...