PND-1186 is a Highly-Specific FAK Inhibitor and Induces Apoptosis
Focal adhesion kinase (FAK) is a tyrosine kinase overexpressed in cancer cells. Especially, FAK plays an important role in the progression of tumors to a malignant phenotype. FAK associates with integrins and modulates various cellular processes including growth, survival, and migration. In particular, PND-1186 is a substituted pyridine reversible...
DMU-212 Possesses Antimitotic, Anti-Proliferative, Antioxidant and Apoptosis Promoting Activities
Resveratrol is a naturally occurring phytoalexin that possesses a wide diversity of anticancer effects. Especially, Resveratrol inhibits multi-kinase enzyme activity and induces apoptosis. In particular, DMU-212 is a Resveratrol analogue containing methoxy groups in place of the hydroxyl groups of the stilbene moiety. DMU-212 inhibits cellular proliferation of A375,...
BI-3802-Induced Polymerization Triggers Degradation of BCL6
PROTAC has been developed to degrade a wide range of clinically relevant targets. These small-molecule degraders engage both the E3 ligase and the target protein to promote the formation of a substrate–drug–ligase ternary complex. Although degraders can show notable efficacy and sustained depletion of targets, some proteins are resistant....
CTPI-2 is a Mitochondrial Citrate Carrier SLC25A1 Inhibitor
Nonalcoholic fatty liver disease (NAFLD) and inflammatory steatohepatitis (NASH) comprise a series of manifestations that span from reversible hepatic steatosis to progressive necroinflammatory and fibrotic disease. There exists a clear association between NASH with obesity, diabetes, and metabolic syndrome. Slc25a1 is a mitochondrial citrate carrier, which belongs to a...
EMI56 is a Superior Mutant EGFR Inhibitor
Receptor Tyrosine Kinases (RTKs) play critical roles in embryogenesis, normal physiology, and several diseases. Epidermal growth factor receptor (EGFR) is a transmembrane protein with cytoplasmic kinase activity that transduces important growth factor signaling from the extracellular milieu to the cell. Furthermore, EGFR common double mutations include 19Del, L858R, and...
SAR-020106 is an ATP-Competitive and Selective CHK1 Inhibitor
Genotoxic antitumor drugs cause DNA damage and activate cell cycle checkpoints, which are required for DNA repair and the maintenance of genomic integrity. The transcription factor p53 is a critical checkpoint protein. As a result, in the presence of damaged DNA, p53 stabilized and activated, causes the upregulation of...
CHDI-390576 is a CNS Penetrant Class IIa HDAC Inhibitor
Class IIa HDAC is a transcriptional corepressor enzyme. They interact with MEF2 transcription factors and the N-CoR, BCoR, and CtBP corepressors. They are capable of shuttling between the cytoplasm and nucleus, hence they are directly linked to cellular signaling networks. Class IIa HDACs found in a wide variety of...