Tag: PI3K

SRX3207 is an Orally Active and First-in-Class Dual Syk/PI3K Inhibitor

Macrophages (MΦ) not only play a role in host defense and tumor growth, metastasis, and immunosuppression. Many studies have demonstrated that targeting the molecular pathways/signaling nodes in the MΦs that regulate the transition of protumorigenic MΦs into anti-tumorigenic MΦs will activate the immune response in cancer. Syk kinase has...

CYH33 is an Orally Active and Highly Selective PI3Kα Inhibitor

PI3Ks are a class of enzymes involved in cell function, such as cell growth, proliferation, differentiation, movement, survival, and intracellular transport. And these cells are relevant to cancer. Specifically, I3K is a kind of related intracellular signal transduction enzymes, which can phosphorylate the 3-hydroxy group of phosphatidylinositol (PtdIns). In...

BAY1082439 is an Orally Active and Selective Balanced PI3Kα/β/δ Inhibitor

Prostate cancer is among the most common malignancy in males. Among the various PI3K isoforms, PTEN-loss-induced prostate cancer in the genetically engineered Pten conditional knockout mouse model predominantly activates the PI3Kβ subunit. However, selective inhibition of PI3Kβ shows no significant anti-tumor efficacy in PTEN-null prostate cancer cell lines. It...

AMG 511 is an Orally Active pan-PI3K Inhibitor

The PI3K signaling network has a central role in several cellular processes critical to the initiation and progression of cancer, including growth, survival, and metabolism. The PI3K family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger that plays a critical role in important cellular functions such as...

BAY1082439 is an Orally Active and Selective PI3Kα/β/δ Inhibitor

Prostate cancer is among the most common malignancy in males. It is also the second leading cause of male cancer-related death in the Western world.  The PI3K pathway is associated with adverse outcomes of prostate cancer. In the Pten conditional knockout mouse model, selective inhibition of PI3Kβ shows no...

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...

PI-828 is a Dual PI3K and Casein Kinase 2 Inhibitor

PI3Ks (phosphatidylinositol 3-kinases) are lipid kinases responsible for the phosphorylation of phosphatidylinositols on the D3 position of their inositol ring. Specifically, The PI3Ks regulate cellular signaling networks. The processes involved these linked to the survival, growth, proliferation, metabolism and specialized differentiated functions of cells. Besides, The subversion of this...