BAM7 is the first potent and selective small molecule activator of BAX, which is a pro-apoptotic BCL-2 family member. It binds the BAX trigger site with an EC₅₀ ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX. BAM7 triggers in vitro BAX oligomerization, BAX-mediated pore formation, and does not interact with the BH3-binding pocket of antiapoptotic proteins or proapoptotic BAK. It induces cell death in a BAX-dependent fashion. It can also induce the biochemical and morphologic features of BAX-mediated apoptosis in Bak^-/- MEFs. BAM7 is selective for the BH3-binding groove at the N-terminal face of BAX and thus may serve as a powerful chemical tool for dissecting the physiologic consequences of direct BAX activation in a variety of homeostatic and pathologic conditions. 

How to Use:

In vitro:  BAM7 was used at 10-30 µM final concentration in vitro and in cellular assays.

In vivo: n/a 

Reference:

1.  1. Gavathiotis E, et al. Direct and selective small-molecule activation of proapoptotic BAX. (2012) Nat Chem Biol. 8(7):639-45.

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