apogossypol

Apogossypol is a semi-synthetic small-molecule BH3 mimic derived from gossypol, a natural polyphenol found in cottonseed. It was specifically engineered to lack the reactive aldehyde groups present in gossypol, which are associated with off-target toxicity, while retaining potent inhibitory activity against anti-apoptotic Bcl-2 family proteins, including Bcl-2, Bcl-XL, and Mcl-1. By binding to the hydrophobic grooves of these proteins, apogossypol prevents them from sequestering pro-apoptotic proteins, thereby triggering the intrinsic apoptotic pathway in cancer cells. Preclinical research has demonstrated its efficacy in inhibiting the growth and proliferation of various malignancies, particularly prostate cancer and hematologic tumors, with a significantly improved safety profile compared to its parent compound.

Brand names

ApoG2ApoG-2ApoG 2

Other names

apogossypoloneapogossypol