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...
TAK-683 is a Potent Metastin/GPR54 Agonist
Metastin/kisspeptin is a 54 amino acid peptide from human placental tissues. It is also the ligand of an orphan G protein-coupled receptor GPR54. GPR54, the KISS1 gene encodes the KISS1 receptor (KISS1R) and expresses in the rodent and human placenta and brain. In this article, we will introduce a...
ARCC-4 is a Highly Potent PROTAC Androgen Receptor Degrader
Androgen receptor (AR) signaling is crucial for normal prostate development. It also drives the growth and survival of prostate cancer cells. AR signaling suppression is a common strategy for treating prostate cancer. Like other occupancy-based inhibitors, the antiandrogen enzalutamide requires high saturating drug concentrations to achieve its clinical benefit....
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...
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...
DC-5163, a GAPDH Inhibitor, Inhibits Glycolysis Pathway and Induces Apoptosis
Cancer cells always exhibit abnormal energy metabolism. Abnormal energy metabolism often leads to an increase in glucose uptake and lactic acid fermentation. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) is an important catalyzing enzyme for glycolysis. GAPDH catalyzes key steps at the center of the glycolysis process. And this process is the convergence...
TL13-12 is a Selective ALK-PROTAC Degrader
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase. ALK is an attractive target for cancer therapies not only for its prominent role in a number of malignancies but also for its scant expression in normal adult tissue. Therapeutic strategies that target ALK may provide ways to further delay...