Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
Wortmannin (SL-2052) is an Orally Active, Selective and Irreversible PI3K Inhibitor
Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ. There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K,...
LY294002, a PI3K Inhibitor, is an Autophagy and Apoptosis Inducer
The phosphatidylinositol-3 OH kinase (PI3K)/Akt signaling pathway contributes to cancer survival, apoptosis, and regulating a variety of cellular processes. In particular, Akt serine/threonine kinase plays a critical role in controlling the balance between cell survival and apoptosis. Dysregulation of this pathway is frequently observed in a variety of tumors,...
PQR530 is an Orally Active and Brain-Penetrant Dual PI3K, mTORC1/2 Inhibitor
Several brain disorders, such as epilepsy, found dysregulation of the PI3K/Akt/mTOR pathway. The PI3K-AKT/mTOR pathway is a central player of intracellular signaling, regulating neuronal survival, growth, and plasticity. Aberrant activation of this signaling pathway drives the progression of malignant tumors. The mutation of growth factor receptors, PI3K, loss of...
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...