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...
PD-161570 is an Inhibitor of FGF-1R, PDGFR, EGFR and c-Src Tyrosine Kinases
Fibroblast growth factors (FGF) are a family of cell-signaling proteins, which are involved in many processes, especially as the key factor of normal development. In addition, the FGFR family consists of a group of four homologous receptor tyrosine kinases. Besides, FGF1 was a member of a family of FGF...
NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity
Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...
CM10 is a Selective Aldehyde Dehydrogenase 1A Family Inhibitor
The aldehyde dehydrogenase (ALDH) superfamily has 19 protein-coding family members with varying tissue or development expression. In addition, ALDHs metabolize endogenous and exogenous aldehydes to their corresponding carboxylic acids to prevent the accumulation of toxic aldehydes. Besides, ALDH1A enzymes are also involved in the biosynthesis of retinoic acid (RA)....
CCT36776 is a PROTAC-based Pirin Protein Degradation Probe
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules. It induces rapid and selective protein degradation, via the proteasome. PROTACs contain two different ligands connected by a linker, one portion of the molecule engages the target protein. While the other, attach via a flexible linker, recruits an E3 ubiquitin ligase to...
ML141 is a Selective, Reversible and Non-competitive Cdc42 GTPase Inhibitor
Cdc42 protein is an essential GTPase that belongs to the Rho/Rac subfamily of Ras-like GTPases. These proteins act as molecular switches to activate downstream components of a biological pathway. CDC42 plays an important role in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Particularly, Overactive Cdc42 implicates...
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...