Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis
Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...
JX06 is a Potent, Selective and Covalent Inhibitor of PDK
Pyruvate dehydrogenase kinase (PDK) is a kinase that can be inactivated by the use of ATP phosphorylation of pyruvate dehydrogenase. Specifically, PDK is relevant to the regulation of the pyruvate dehydrogenase complex with pyruvate dehydrogenase as the first component. Besides, PDK acts as a molecular switch to reduce mitochondrial...
RA375, a RPN13 Inhibitor, Activates UPR Signaling, ROS Production and Apoptosis
Rpn13 is a known component of the proteasome. Especially, Rpn13 binds ubiquitin-like domains of the UBL/UBA family of ubiquitin receptors. Rpn13, as an ubiquitin receptor, offers a docking position for ubiquitinated substrate. RA375 is a RPN13 inhibitor. Treatment with RA375 causes a rapid and profound accumulation of high molecular weight polyubiquitinated proteins. RA375...
TCH-165, a Proteasome Assembly Modulator, Regulates the Dynamic Equilibrium between the 20S and 26S Proteasome Complexes
Intrinsically disordered proteins (IDPs) involves a number of multiple regulatory and signaling events. In addition, the accumulation of IDPs results in some harmful signals happening in the pathogenesis of many human diseases. The proteasome contains different include active complexes (such as the 26S proteasome) and a weakly active complex: the...