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.
CAS Number: 331244-89-4
Molecular Weight: 405.47
Chemical Name: (E)-4-(2-(2-ethoxyphenyl)hydrazono)-3-methyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol- 5(4H)-one
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
BAM7 was used at 10-30 µM final concentration in vitro and in cellular assays.
- 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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