BAM7 --- BAX Activator

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.

Product information

CAS Number: 331244-89-4

Molecular Weight: 405.47

Formula: C21H19N5O2S

Synonym:

BAM 7

BAM-7

SML 0641

Chemical Name: (E)-4-(2-(2-ethoxyphenyl)hydrazono)-3-methyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol- 5(4H)-one

Smiles: CC1=NN(C(=O)C1=NNC1=CC=CC=C1OCC)C1=NC(=CS1)C1C=CC=CC=1

InChiKey: KOCVKGYKBLJEPK-LYBHJNIJSA-N

InChi: InChI=1S/C21H19N5O2S/c1-3-28-18-12-8-7-11-16(18)23-24-19-14(2)25-26(20(19)27)21-22-17(13-29-21)15-9-5-4-6-10-15/h4-13,23H,3H2,1-2H3/b24-19+

Technical Data

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

In Vitro:

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

References:

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

Products are for research use only. Not for human use.

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