Category: Cancer

XY028-140 is a Selective CDK4 and CDK6 PROTAC Degrader

CDKs (Cyclin-dependent kinases) are the families of protein kinases first discovered for their role in regulating the cell cycle. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase. The four major mechanisms...

Inupadenant is an Orally Active and Highly Selective A2A Receptor Antagonist

Adenosine receptors (AR), including P1 purinergic receptors, belong to G protein-coupled receptors (GPCR). Specifically, Adenosine is an autogenous acid in all tissues and body fluids. Besides, AR contains four subtypes, A1, A2A, A2B, and A3. They are activated by extracellular adenosine and play a central role in a wide...

AUTAC4 is a Mitochondria-Targeting Autophagy-Targeting Chimera (AUTAC)

A novel chimeric molecule, namely autophagy-targeting chimera (AUTAC), is the first degrader using the autophagy mechanism. AUTAC consists of a guanine tag and a specific binder of an intracellular target of interest. In addition, AUTAC can penetrate cell membranes, and degrade fragmented mitochondria as well as proteins. Mitochondria not...

GSK973 is a Highly Selective BET BD2 Inhibitor

The bromodomain and extra-terminal (BET) family of proteins are epigenetic readers of chromatin. The two tandem bromodomains (BD1 and BD2) of each of the four proteins (BRD2, 3, 4, and T) recognize and bind to specific acetylated-lysine residues of histone tails and non-histone proteins. They play a major role...

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...

MR837 is an Inhibitor of NSD2-PWWP1

NSD2 (nuclear receptor-binding SET domain-containing 2) is a protein lysine methyltransferase. It belongs to the NSD family, which also includes NSD1 and NSD3, and that predominantly mono- and dimethylates lysine 36 of histone 3 (H3K36). NSD2 is an oncoprotein that is aberrantly expressed, amplified, or somatically mutated in multiple...