CCT36776 is a PROTAC-based Pirin Protein Degradation Probe
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules. It induces rapid and selective protein degradation, via the proteasome. PROTACs contain two different ligands connected by a linker, one portion of the molecule engages the target protein. While the other, attach via a flexible linker, recruits an E3 ubiquitin ligase to...
ML141 is a Selective, Reversible and Non-competitive Cdc42 GTPase Inhibitor
Cdc42 protein is an essential GTPase that belongs to the Rho/Rac subfamily of Ras-like GTPases. These proteins act as molecular switches to activate downstream components of a biological pathway. CDC42 plays an important role in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Particularly, Overactive Cdc42 implicates...
COTI-2 is an Orally Available Mutant p53 Activator
TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...
Niraparib is an Orally Active PARP Inhibitor
Poly (ADP-ribose) polymerases (PARPs) are a family of related enzymes. PARP shares the ability to catalyze the transfer of ADP-ribose to target proteins. PARP plays an important role in various cellular processes, including modulation of chromatin structure, transcription, replication, recombination, and DNA repair. Niraparib (MK-4827) is a potent PARP...
TVB-3166 is an Orally Active and Selective FASN Inhibitor
Fatty acid synthases (FASN) are homodimers and multifunctional enzymes that catalyze palmitate biosynthesis in NADPH dependent reactions. FASN plays an important role in tumor cell biology and therapeutic response of various cancer types. In fatty acid synthesis, FASN consumes NADPH, acetyl coenzyme A and malonyl coenzyme A. The consumption of...
PTC-028 is an Inhibitor of BMI-1 with Activity in Ovarian Cancer
Epithelial ovarian cancers are the most common type of ovarian cancer. BMI-1 over-expresses in epithelial ovarian cancer. Targeting BMI-1 sensitizes a variety of cancer cells to chemo-therapeutics. The B cell-specific moloney murine leukemia virus integration site 1 (Bmi-1) is a transcriptional receptor of the polycomb gene family. BMI-1 involves...
CFI-402257 is a Highly Selective and Oral Active Inhibitor of Mps1/TTK
The spindle assembly checkpoint (SAC) is important for cell survival. Its inactivation generates lethal genomic instability in cancer cells. Inhibition of SAC signaling through targeting of Mps1 has provided an indication of the feasibility of such an approach. Mps1 is also an essential, dual-specificity kinase that functions as an...