This peptide, generated from the BH3 domain of Bak (Flu-BakBH3), has been shown to have high-affinity binding to a surface pocket of the Bcl-XL protein that is required for its death antagonist function.
BH3I-2' is a cell-permeable BH3 mimetic. BH3I-2' induces apoptosis by specifically preventing BH3 domain-mediated interactions between pro-apoptotic and anti-apoptotic members of the Bcl-2 family, thereby blocking the interaction between Bcl-x and BakBH3 by targeting the Bcl-x binding pocket.
JY-1-106 is a BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak.
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide that acts as a direct activator of Bak with a Kd of 26 nM. This peptide binds Bcl-2, localizes to mitochondria, and induces cytochrome C release.