Tag: Akt

CAY10404 is a Highly Selective COX-2 Inhibitor

Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...

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...

AZA1 is a Potent Dual Inhibitor of Rac1 and Cdc42

Prostate cancer is the leading cause of cancer and the second leading cause of cancer-related deaths in men. Rho GTPases such as Rac, Cdc42, and RhoA are signaling proteins. They regulate cytoskeleton organization, cell cycle progression, cell survival, and migration directly contributing to tumor growth and progression. Cdc42 additionally...

MK-2206 is an Orally Active and Selective Allosteric Akt Inhibitor

Nasopharyngeal carcinoma (NPC) is a squamous cell carcinoma arising from the epithelium lining of the posterior nasopharynx. In a word, NPC causes very serious health problems in these areas. NPC is highly sensitive to radiation and chemotherapy. However, even with combined radiation and chemotherapy treatment, the prognosis for the...

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...

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...