High affinity and selective activator of Bax (Ki
= 43.3 nM). Binds to the S184 binding pocket to block Bax phosphorylation. Does not bind to other Bcl-2 family members, including Bcl-2, Bak and Bid. Facilitates Bax insertion into the mitochondrial membrane and promotes Bax-dependent cytochrome c release. Induces apoptosis in lung cancer cell lines expressing high levels of Bax selectively over normal cells expressing low levels of Bax. Represses tumor growth of A549 lung cancer xenografts in mice.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Small-molecule Bax agonists for cancer therapy.
Xin M, Li R, Xie M et al.