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...
Wortmannin (SL-2052) is an Orally Active, Selective and Irreversible PI3K Inhibitor
Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ. There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K,...
ARQ 531 (MK-1026) is a Reversible Non-Covalent and Orally Active BTK Inhibitor
Bruton’s tyrosine kinase (abbreviated Btk or BTK) is a tyrosine kinase that is encoded by the BTK gene in humans. BTK, a kinase expressed in B cells and bone marrow cells, has a well-characterized important role in B cells, vital role in B cells highlighted by the human primary...
Sorafenib (Bay 43-9006) is an Orally Active Raf Inhibitor
The Raf family consists of three members: A-Raf, B-Raf, and Raf-1. Ras/RAF/MEK extracellular signal-regulated kinase (ERK) pathway is relevant to the control of many basic cellular processes, including proliferation, survival, and differentiation. Specifically, Raf-1 and B-Raf can form heterodimers, which may be important for cell transformation. RAF protein is...
Cabozantinib is a potent Multiple Receptor Tyrosine Kinases (RTKs) Inhibitor
Receptor tyrosine kinases (RTKs) are high-affinity cell surface receptors for many polypeptide growth factors, cytokines, and hormones. Specifically, RTKs are part of a larger family of protein tyrosine kinases. RTKs are key regulators of normal cellular processes. Besides, it plays a key role in the development and progression of...
SN-38 (NK012) is an Active Metabolite of the Topoisomerase I Inhibitor Irinotecan
DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. Top1 binds supercoiled DNA, nicks a DNA strand allowing its rotation around the intact strand, and then relegates the DNA. Camptothecins bind and stabilize the Top1-DNA cleavage complexes, thus...