CYD-2-11 is a novel potent, selective Bax agonist that targets the structural pocket proximal to S184 in the C-terminal region of Bax (Ki=34.1 nM).
CYD-2-11 shows no affinity for other Bcl-2 family members.
CYD-2-11 directly activates Bax proapoptotic activity by inducing a conformational change enabling formation of Bax homooligomers in mitochondrial membranes.
CYD-2-11 suppresses malignant growth without evident significant toxicity to normal tissues in mutant KRAS-driven lung cancer models.
CYD-2-11 displays strong synergistic activity and overcomes rapalog resistance combined with RAD001.
