DT-061 is an Orally Active PP2A Activator
Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...
APS-2-79 is a KSR-Dependent Antagonist of RAF-Mediated MEK Phosphorylation
Deregulation of the Ras-MAPK pathway is an early event in many different cancers and a key driver of resistance to targeted therapies. Kinase suppressor of Ras (KSR) is a MAPK scaffold. KSR exhibits allosteric regulation through dimerization with RAF. In this study, researchers developed a class of compounds that...
MS432 is a Highly Selective PROTAC Degrader for MEK1 and MEK2
Chemical induced protein knockdown via the proteolysis targeting chimera (PROTAC) technology is a promising approach to target dysregulated proteins. Moreover, MEK1/2 proteins are the only RAF substrates. MEK1/2 proteins are the crucial “gatekeepers” of ERK activity. The classic RAS-RAF-MEK-ERK signaling pathway is common in mammals, plays critical roles in...