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...
MPT0G211 is an Orally Active and Selective HDAC6 Inhibitor
Alzheimer’s disease (AD) is one of the most common neurodegenerative diseases, accounting for more than 80% of dementia cases worldwide. AD leads to the progressive loss of mental capacity and behavior, with a functional decline in the ability to learn. HDAC6 belongs to the HDAC family, and its structure contains...
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...
MSN-125 is a Potent Bax and Bak Oligomerization Inhibitor
Aberrant apoptosis can lead to acute or chronic degenerative diseases. Apoptosis largely divides into two pathways ultimately leading to caspase activation and subsequent cellular disintegration. Extracellular signals activating death receptors triggers the extrinsic pathway, and intracellular stress activates the intrinsic pathway. It largely regulated at the mitochondrial outer membrane...