Tag: PI3K

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...

Alpelisib is a Selective and Orally Active PI3Kα Inhibitor for Metastatic Breast Cancer

Phosphatidylinositol-3-kinases (PI3Ks) are a family of important lipid kinases. PI3Ks are important in controlling the signaling pathways involved in cell proliferation, motility, cell death, and cell invasion. Moreover, PI3Ks control and deliver cellular signals in the PI3K/Akt/mTOR pathway by phosphorylating phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) on the...

CGS 15943 is an Orally Active Adenosine Receptor Antagonist

Hepatocellular carcinoma (HCC) is primary liver cancer and the third most common cause of cancer mortality worldwide. CGS 15943 blocks proliferation in hepatocellular carcinoma (HCC) and pancreatic cancer adenocarcinoma (PDAC) cell lines by inhibiting the PI3K/Akt pathway. Researchers test the adenosine A2 receptor antagonist CGS 15943 for cerebroprotective activity in...