Birinapant (TL32711), a Bivalent Smac Mimetic, is an Antagonist for XIAP and cIAP1
XIAP is a protein that prevents apoptosis. XIAP is a member of apoptosis protein family (IAP) inhibitors. Specifically, IAP blocks cell death in vitro and in vivo by inhibiting different caspases. The caspase inhibitory activity of XIAP is negatively regulated by at least two XIAP interacting proteins XAF1 and...
Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...
Elimusertib is an Orally Available and Selective ATR Inhibitor
TM serine/threonine kinase (ATM) is a serine/threonine-protein kinase and can be recruited and activated by DNA double-strand breaks. Specifically, ATM phosphorylates several key proteins. These proteins initiate the activation of DNA damage checkpoints, leading to cell cycle arrest, DNA repair, or apoptosis. Besides, ATM belongs to the superfamily of...
DMU-212 Possesses Antimitotic, Anti-Proliferative, Antioxidant and Apoptosis Promoting Activities
Resveratrol is a naturally occurring phytoalexin that possesses a wide diversity of anticancer effects. Especially, Resveratrol inhibits multi-kinase enzyme activity and induces apoptosis. In particular, DMU-212 is a Resveratrol analogue containing methoxy groups in place of the hydroxyl groups of the stilbene moiety. DMU-212 inhibits cellular proliferation of A375,...
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...
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...