Tag: DNA-PK

PIK-75 is a Reversible DNA-PK and p110α Selective Inhibitor

PI3Ks catalyze the phosphorylation of the D-3 position of the inositol headgroup of phosphatidylinositol leading to the synthesis of second messengers PtdIns3P, PtdIns(3,4)P2, PtdIns(3,5)P2 and PtdIns(3,4,5)P3. The p110α and p110β are the main forms in insulin target tissues. Especially, p110α isoform (PIK3CA) plays the predominant role in insulin signaling....

PI-103 is a Potent PI3K and mTOR Inhibitor

The phosphatidylinositide 3-kinase family possesses 15 members. those members consist of four distinct classes as a basis on their structure and biological properties. As we all know, this highly conserved family of enzymes involves various aspects of cellular homeostasis and exists a decline in a number of pathophysiologic conditions....

CC-223 is an Orally Bioavailable mTOR Kinase Inhibitor

mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTORC1 is a master regulator of cell growth and metabolism. mTORC1 positively regulates cell growth and proliferation. mTORC2 regulates cytoskeletal organization. CC-223 is a potent mTOR kinase inhibitor with an IC50 of 0.016 μM. CC-223 is...

KU-0060648 is a Dual PI3K and DNA-PK Inhibitor

DNA double-strand breaks (DSBs) are the principal cytotoxic lesions induced by topoisomerase II poisons. And DSB inhibitors are widely applied in the treatment of a variety of human solid malignancies and leukemia. Cells defective in DSB repair by virtue of the inactivation of a component of the NHEJ pathway...