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...
DT2216 is a Selective PROTAC Degrader of BCL-XL
BCL-XL is a member of the Bcl-2 protein family and a transmembrane molecule in mitochondria. Specifically, it acts as an anti-apoptotic protein by blocking the release of mitochondrial contents such as cytochrome c. Besides, BCL-XL is a well-validated cancer target and eventually leads to caspase activation and eventually programmed...
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...
XZ739 is a PROTAC BCL-XL Degrader
PROTAC is an emerging therapeutic modality. PROTAC is a feasible solution to reduce platelet toxicity associated with BCL-XL inhibition. BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance. As a result, BCL-XL is an attractive target for cancer treatment. Specifically, XZ739 is a CRBN-dependent BCL-XL degrader. XZ739,...