FPA-124 is a Selective Akt Inhibitor and Induces Apoptosis
Copper complexes play an important role in the active sites of a large number of metalloproteins in biological systems. Copper complexes also have a potential application for numerous catalytic processes in living organisms. In addition, copper complexes involve electron transfer reactions or activation of some antitumor substances. In this...
PI-828 is a Dual PI3K and Casein Kinase 2 Inhibitor
PI3Ks (phosphatidylinositol 3-kinases) are lipid kinases responsible for the phosphorylation of phosphatidylinositols on the D3 position of their inositol ring. Specifically, The PI3Ks regulate cellular signaling networks. The processes involved these linked to the survival, growth, proliferation, metabolism and specialized differentiated functions of cells. Besides, The subversion of this...
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...
UK 356618 is a Selective MMP-3 Inhibitor
Matrix metalloproteinase-3 (MMP-3) plays an important role in the pathology of rheumatoid arthritis (RA) and ankylosing spondylitis (AS). MMP-3 contains a signal peptide, a pro-domain, a catalytic domain, a hinge domain, and a hemopexin domain. Besides, the signal peptide is cleaved off during the secretion process and pro-domain is...
DRF-1042 is an Orally Active DNA topoisomerase I Inhibitor
Inhibitors of the enzyme topoisomerase I are cytotoxic for tumor cells because of their ability to cause DNA damage. Specifically, DNA Topoisomerase I (Top1) is one main cellular factor controlling topological homeostasis. Top1 activity can relax negative supercoils by cutting one of the DNA strands. This can create a...
TK216 is an ETS Transcription Factor Inhibitor for Treatment of Ewing Sarcoma
The erythroblastosis virus E26 transformation specific (ETS)-transcription factors family comprises 28 proteins sharing a conserved DNA-binding domain. Transcription factors are difficult to target due to their non-enzymatic mechanisms of action. Transcription factors often complex with RNA helicases; these enzymes are key regulators of cellular transformation in cancer. EWS-FLI1 is...
MG-277, a PROTAC Molecular Glue, Exhibits Anti-cancer Activity by Inhibiting GSPT1
Proteolysis targeting chimeras (PROTACs) induce protein degradation. A typical PROTAC small-molecule degrader consists of three essential components: a ligand that binds the protein of interest, a second ligand that binds to and recruits an E3 ligase degradation complex, and a linker tethering the two ligands together. MD-222, a bona...