Home Apoptosis Bcl-2 activator BAM7

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BAM7 Bcl-2 activator

Cat.No.S7105

BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.
BAM7 Bcl-2 activator Chemical Structure

Chemical Structure

Molecular Weight: 405.47

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Quality Control

Batch: S710501 DMSO]2 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%
99.88

Chemical Information, Storage & Stability

Molecular Weight 405.47 Formula

C21H19N5O2S

 Storage (From the date of receipt)
CAS No. 331244-89-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOC1=CC=CC=C1N=NC2=C(NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C

Solubility

In vitro
Batch:

DMSO : 2 mg/mL ( (4.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

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/IC50/Ki
Bax [1]
3.3 μM
In vitro
BAM7 directly binds the previously uncharacterized BH3-binding groove at the N-terminal face of BAX. This compound is selective for the BH3-binding groove at the N-terminal face of BAX. It directly interacts with BAX at the very surface used by the BIM BH3 helix to trigger BAX activation. This chemical results in functional BAX activation. It 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. This compound triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death. It selectively induces BAX-mediated apoptosis by triggering the hallmark features of intracellular BAX activation. This chemical only kills the cell line that contains BAX, eliciting the biochemical and morphologic features of BAX-mediated apoptosis. [1]
Kinase Assay
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 this compound 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.
References

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