SD-1029 is a JAK2/STAT3 Activation Inhibitor
Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. JAK includes JAK1, JAK2, JAK3 and TYK2. JAK serves as the cytoplasmic signaling components of cytokine receptors and are activated through cytokine-mediated trans-phosphorylation. The pseudokinase domain of JAKs is crucial...
Rucaparib is a PARP Inhibitor
PARP is a family of proteins involved in many cellular processes, such as DNA repair, genomic stability, and programmed cell death. At least 18 members of the PARP family are encoded by different genes and have homology in conserved catalytic domains. Specifically, PARPs play an important role in various...
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...