Category: Glioma

M2698 is an Orally Active, ATP-Competitive, Selective, Dual p70S6K and Akt Inhibitor

The disorder of PI3K/Akt/mTOR (PAM) signaling pathway occurs in about 30% of human cancers, making it a reasonable target for new therapies. Specifically, the pathway is an important regulator of growth, proliferation, and metabolism. However, some PAM pathway inhibitors, such as Rapamycin complex (mTORC) rapalogs, cause the impairment of...

PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket

Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...

MN58b is a Selective Choline Kinase α Inhibitor

Choline kinase (CHK) catalyzes the phosphorylation of choline by ATP in the presence of Mg2+, yielding phosphocholine. This enzyme step commits choline to the Kennedy pathway for the biosynthesis of phosphatidylcholine, the major phospholipid constituent in biomembranes. Phosphatidylcholine has an essential structural function as well as serving as a...