BAM7

Catalog No.S7105

BAM7 Chemical Structure

Molecular Weight(MW): 405.47

BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

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Biological Activity

Description BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.
Features Does not interact with the BH3-binding pocket of antiapoptotic proteins or proapoptotic BAK and induces cell death in a BAX-dependent fashion.
Targets
Bax [1]
3.3 μM
In vitro

BAM7 directly binds the previously uncharacterized BH3-binding groove at the N-terminal face of BAX. BAM7 is selective for the BH3-binding groove at the N-terminal face of BAX. BAM7 directly interacts with BAX at the very surface used by the BIM BH3 helix to trigger BAX activation. BAM7 results in functional BAX activation. BAM7 triggers the conversion of BAX from monomer to oligomer in a dose- and time-responsive manner, the kinetics of which approach saturation at a 1:8 dose ratio of BAX:BAM7. BAM7 triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death. BAM7 selectively induces BAX-mediated apoptosis by triggering the hallmark features of intracellular BAX activation. BAM7 only kills the cell line that contains BAX, eliciting the biochemical and morphologic features of BAX-mediated apoptosis. [1]

Protocol

Kinase Assay:[1]
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Fluorescence polarization binding assays:

Direct binding curves are first generated by incubating FITC-BIM SAHB (50 nM) with serial dilutions of fulllength BAX, BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC or BAKΔC and fluorescence polarization measured at 20 minutes on a SpectraMax M5 microplate reader. For competition assays, a serial dilution of small molecule or acetylated BIM SAHB (Ac-BIM SAHB) is combined with FITC-BIM SAHB (50 nM), followed by the addition of recombinant protein at ~EC75 concentration, as determined by the direct binding assay (BAX, BAKΔC: 500 nM; BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC: 200 nM). Fluorescence polarization is measured at 20 minutes and IC50 values calculated by nonlinear regression analysis of competitive binding curves using Prism software.
Cell Research:[1]
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  • Cell lines: MEFs
  • Concentrations: ~15 μM
  • Incubation Time: 24 h
  • Method: MEFs (2.5 × 103 cells per well) are seeded in 96-well opaque plates for 18-24 h and then incubated with serial dilutions of BAM7, ANA-BAM16 or vehicle (0.15% (v/v) DMSO) in DMEM at 37 °C in a final volume of 100 μL. Cell viability is assayed at 24 h by addition of CellTiter-Glo reagent according to the manufacturer’s protocol, and luminescence is measured using a SpectraMax M5 microplate reader. Viability assays are performed in at least triplicate, and the data are normalized to vehicle-treated control wells.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL (4.93 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 405.47
Formula

C21H19N5O2S

CAS No. 331244-89-4
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID