dTRIM24 is a Selective PROTAC Degrader of TRIM24
TRIM24 is a multidomain protein characterized as a co-regulator of transcription. Especially, dTRIM24 acts as a chemical probe of an emerging cancer dependency. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. TRIM24 has been posited as a dependency in numerous cancers,...
PU02 is an Allosteric Antagonist of 5-HT3 Receptor
Cancer is a usual disease and a leading cause of death in the world. Therefore, developing new agents specifically targeting cancer cells has achieved more and more researches. As it is widely believed that cancer can be treated by inducing tumor cells to undergo senescence or apoptosis, screening for...
Z-LEHD-FMK is a Selective and Irreversible Inhibitor of Caspase-9
TRAIL is a potent inducer of apoptosis of transformed and cancer cells but not of most normal cells. TRAIL induces apoptotic death on binding to either of two proapoptotic TRAIL receptors, TRAIL R1 or TRAIL R2. Moreover, normal cells may resistant to TRAIL because of expressing higher levels of...
CAY10404 is a Highly Selective COX-2 Inhibitor
Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...
ZZW-115, a NUPR1 Inhibitor, Possesses Anticancer Activity via Inducing Necroptosis and Apoptosis
NUPR1 is an intrinsically disordered protein (IDP) with an entirely disordered conformation. It binds to DNA in a manner similar to other chromatin proteins to control the expression of gene targets. At the cellular level, NUPR1 participates in many cancer-associated processes, including cell-cycle regulation, apoptosis, senescence, cell migration and...
BM-1197 is a Potent and Selective Dual Bcl-2/Bcl-xL Inhibitor
Bcl-2 and Bcl-xL are critical regulators of apoptosis. The pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising strategy for cancer treatment. In addition, BM-1197 is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL. BM-1197 binds to Bcl-2 and Bcl-xL proteins with Ki values less than 1...
SBP-0636457, a SMAC Mimetic, is an IAP Antagonist
Cancer cells regularly acquire resistance to programmed cell death, or apoptosis, which not only supports cancer progression but also leads to resistance to therapeutic agents. In this study, researchers focus their research on the inhibitor of apoptosis protein (IAP) family. IAPs are a disparate group of proteins that all...