TAS-119 is a Selective and Orally Active Aurora A Inhibitor
Aurora kinases represent a serine/threonine kinase family crucial for cell-cycle control. In particular, Aurora kinases are important and indispensable in multiple steps of mitotic progression. Specifically, Aurora kinase A acts primarily during the prophase of mitosis. Overexpression of Aurora A in HeLa cells attenuates the antiproliferative activity of Paclitaxel....
PF-06843195 is a Selective PI3Kα Inhibitor
Phosphoinositide 3-kinases (PI3Ks) can catalyze the synthesis of the phosphatidylinositol (PI) second messengers, including PI(3)P (PIP), PI(3,4)P2 (PIP2), and PI(3,4,5)P3 (PIP3). The PI3K lipid kinase family contains three classes based on sequence homology. Class, I PI3Ks are further divided into class IA (PI3Kα, PI3Kβ, and PI3Kδ) and class IB...
ML390 is a Potent DHODH Inhibitor
Dihydrowhey dehydrogenase (DHODH) catalyzes the fourth enzymatic step of pyrimidine biosynthesis, namely, ubiquinone mediated oxidation of dihydrowhey acid to whey acid. Specifically, DHODH is a mitochondrial protein located on the outer surface of the mitochondrial inner membrane (IMM). Inhibitors of the enzyme are used to treat autoimmune diseases such...
Barasertib, a Pro-Drug of Barasertib-hQPA, is a Highly Selective Aurora B Inhibitor
Aurora kinases play an important role during mitosis for chromosome alignment, segregation, and cytokinesis. Selective Targeting of Aurora B kinase may be a promising therapeutic approach for the treatment of a range of malignancies. In this study, researchers explored the effect of Barasertib. In particular, Barasertib is a highly...
PR-619 is a Broad-Range DUB Inhibitor
Ubiquitination is a post-translational modification where the polypeptide ubiquitin is attached to lysine residues of substrate proteins. This process is reversible, and ubiquitin removal is orchestrated by a large family of deubiquitinating enzymes (DUBs). DUBs fall into six subfamilies based on sequence and domain similarity. Ubiquitination and deubiquitination together...
NSC 33994 is a Selective JAK2 Inhibitor
Janus kinases (JAK) play a crucial role in cytokine-mediated signal transduction. Activated JAKs tyrosine autophosphorylate and phosphorylate specific tyrosine residues on the C-terminal end. This results in the recruitment and activation of the STAT proteins. Activated STATs subsequently translocate into the nucleus where they alter specific gene transcription patterns....
AKI603 is an Aurora Kinase A Inhibitor with Anti-tumor Activity
Chemoresistance is a major cause of cancer treatment failure. Tumor-initiating cells (TIC) have attracted a considerable amount of attention due to their role in chemoresistance and tumor recurrence. The inhibition of AurA kinase by AKI603 abrogates the epirubicin-induced enrichment of TICs.In this study, researchers evaluated the small molecule Aurora...