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...
Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...
IACS-010759 is a Potent Inhibitor of Complex I of OXPHOS
Oxidative phosphorylation (OXPHOS) is a metabolic pathway in which cells use enzymes to oxidize nutrients. So it releases the chemical energy stored in nutrients to produce adenosine triphosphate (ATP). Besides, mitochondria are key players in the production and regulation of cellular bioenergy. Most adenosine triphosphate molecules are produced by...
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...
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...
Everolimus (RAD001), a Rapamycin Derivative, is a Selective and Orally Active mTOR1 Inhibitor
mTOR is a member of the phosphatidylinositol 3-kinase related kinase family of protein kinases. Meanwhile, mTOR is linked to other proteins and serves as the core component of two different protein complexes, mTOR complex 1 and mTOR complex 2. They regulate different cellular processes. Nonetheless, mTOR C1 phosphorylates p70...
Ruxolitinib (INCB018424) is an Orally Active JAK1 and JAK2 Inhibitor
The myeloproliferative neoplasms (MPNs) are a group of related clonal diseases probably arising from hematopoietic progenitor or stem cells. Patients with MPNs have an increased risk of thrombotic and bleeding complications and disease progression to acute myeloid leukemia. JAK2 is a member of the JAK family of cytoplasmic tyrosine...