AZD4635 (HTL1071) is a Selective and Orally Active A2AR Antagonist

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes (A1R, A2AR, A2BR, A3R) have been cloned and identified in different tissues. Adenosine receptors play an important role in sleep, the development of cancers and hearing...

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,...

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...