DCH36_06 is a Selective p300/CBP Inhibitor
Histone acetyltransferases (HATs) are epigenetic enzymes that relieve transcriptional repression by preferentially acetylation of ε-amino group of lysine residues on histones. In general, HATs are crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells. HATs can be grouped into at least five different subfamilies (HAT1, Gcn5/PCAF, MYST, p300/CBP,...
UK122 is a Selective Urokinase-Type Plasminogen Activator (uPA) Inhibitor
Urokinase, also known as urokinase-type plasminogen activator (uPA), is a serine protease found in humans and other animals. Specifically, UPA is relevant to tissue remodeling and cell migration. The active form of uPA binds to its high-affinity receptor on the cell surface, and specific inhibitors can regulate its enzyme...
Pelcitoclax (APG-1252) is a Bcl-2/Bcl-xl Inhibitor with Antineoplastic and Pro-Apoptotic Effects
Bcl-2 (B-cell lymphoma 2) is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). Particularly, the Bcl-2 and Bcl-xl...
Nimotuzumab is a Humanized IgG1 Monoclonal Antibody Targeting EGFR
The epidermal growth factor receptor (EGFR) is a transmembrane protein. The dimerization of EGFR stimulates the activity of intracellular protein tyrosine kinase. Therefore, several tyrosine (y) residues in the C-terminal domain of EGFR undergo autophosphorylation. These include y992, y1045, y1068, y1148, and y1173, as shown in the adjacent chart....
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...
GGTI-2154 is a Selective Geranylgeranyltransferase I (GGTase I) Inhibitor
The Ras superfamily of low molecular weight GDP/GTP-binding GTPases is critical in the regulation of many important biological events. They include the cell division cycle, survival and death, differentiation, and development. These GTPases also show a relation with oncogenesis, Ras and Rho proteins mediate malignant transformation, invasion, and metastasis....
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...