Pimasertib is a Highly Selective and ATP non-Competitive Allosteric Inhibitor of MEK1/2
The RAS/RAF/MEK/MAPK and the PTEN/PI3K/AKT/mTOR pathways are key regulators of proliferation and survival in human cancer cells. RAF is a serine/threonine kinase that activates downstream signals in response to activated GTP-bound RAS by phosphorylating MEK (MEK1 and MEK2). They in turn phosphorylate and activate MAPK (or ERK1 and ERK2)....
IACS-15414 is an Orally Active SHP2 Inhibitor
Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved structure and function. It has emerged as a key downstream regulator of several receptor tyrosine kinases (RTKs) and cytokine...
BI-3406 is an Orally Active and Selective KRAS and SOS1 Interaction Inhibitor
KRAS functions as a molecular switch, cycling between inactive (GDP-bound) and active (GTP-bound) states to transduce extracellular signals via cell-surface receptors. KRAS signaling occurs through engagement with effector proteins that orchestrate intracellular signaling cascades regulating tumor cell survival and proliferation. Mutations in the KRAS gene occur in approximately one of seven...
Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...
IACS-13909 is a Selective and Orally Active SHP2 Inhibitor
Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases. SHP2 suppresses signaling through the MAPK pathway. Furthermore, SHP2 inhibition has demonstrated tumor growth inhibition in receptor tyrosine kinases-activated cancers. In this study, researchers report the discovery of IACS-13909. IACS-13909 is...
APS6-45, an Orally Active Tumor-Calibrated Inhibitor, Inhibits RAS/MAPK Signaling
Medullary thyroid cancer is a form of thyroid carcinoma which originates from the parafollicular cells, which produce the hormone calcitonin. Synthetic tailoring of approved drugs for new indications is often difficult, as the most appropriate targets may not be readily apparent and therefore few roadmaps exist to guide chemistry....
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...