Molecular Weight: | 405.47 |
Formula: | C21H19N5O2S |
Purity: | ≥98% |
CAS#: | 331244-89-4 |
Solubility: | DMSO up to 100 mM |
Chemical Name: | (E)-4-(2-(2-ethoxyphenyl)hydrazono)-3-methyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one |
Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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. 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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