Flavopiridol (Alvocidib) is a pan CDK Inhibitor
The cyclin-dependent kinases (CDKs) are serine/threonine protein kinases. And it exhibits drives force behind the cell cycle and cell proliferation. CDKs contain at least a catalytic subunit (CDK) and a regulatory subunit (cyclin). To date, at least 10 CDKs and 15 cyclins have been identified. Once activation, CDKs phosphorylate...
GSK2606414 is an Orally Available PERK Inhibitor
PERK (Protein kinase R (PKR)-like endoplasmic reticulum kinase) is a type I endoplasmic reticulum transmembrane protein. Generally, PERK contains a stress-sensing domain facing the endoplasmic reticulum lumen and a cytosolic kinase domain. Interestingly, PERK is a major component of the unfolded protein response (UPR), which promotes the adaptation of...
YUM70, a Selective GRP78 Inhibitor, Induces ER Stress-Induced Apoptosis
GRP78 (Glucose-regulated protein, 78 kDa) is a key regulator of endoplasmic reticulum (ER) stress signaling. In this study, researchers describe the discovery of a series of GRP78 inhibitors. YUM70 is an ER stress inducer and kills cells by activating the apoptosis pathway. Especially, YUM70 treatment induces ER stress and...
ADPM06 is a Novel Nonporphyrin Photodynamic Therapeutic (PDT) Sensitizer and Induces Apoptosis
Photodynamic therapeutic (PDT) is an established treatment modality for cancer. It utilizes a photosensitive compound accompanied by low-energy light of a specific wavelength. The combination of these two independently nontoxic components produces extensive cellular, vascular, and tissue damage in an oxygen-dependent manner, via reactive oxygen species (ROS) generation, resulting in...
GSK621 is a Specific AMPK Activator, Inducing Autophagy and Apoptosis
AMPK is an enzyme, which plays a role in cell energy homeostasis. It mainly activates glucose and fatty acid uptake and oxidation when the cell energy is low. Specifically, AMPK is a major regulator of cell metabolism, which can exert its carcinogenic or antitumor activities. Besides, the activation of...
RA-9 is a Selective Proteasome-Associated DUBs Inhibitor
The ubiquitin-proteasome-system (UPS) is responsible for most of the intracellular protein degradation in eukaryotes. UPS consists of three components: the proteasomes, the ubiquitin conjugating system, and the deubiquitinating enzymes (DUBs). DUBs deconjugate ubiquitin from targeted proteins and this step is essential for protein degradation. The de-ubiquitination is required for...