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BAM7

In stock
Catalog No.
A3218
BAX activator,direct and selective
Grouped product items
SizePriceStock Qty
5mg
$90.00
In stock
10mg
$150.00
In stock
25mg
$337.00
In stock

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Email: [email protected]

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Background

BAM7 is a direct and selective activator of BAX with IC50 value of 3.3uM [1].

In the competitive fluorescence polarization assay (FPA), BAM7 competes with FITC–BIM SAHB for BAX binding site(BH3) in a dose dependent manner. BAM7 shows no antiapoptotic or BAKΔC competitive binding interactions even at 50 μM dosing, revealing a remarkable selectivity of BAM7 for BAX. The interaction between BAM7 and BAX at the very surface induces the characteristic structural changes that yield functional BAX oligomerization. In the in vitro assay, BAM7 induces BAX-dependent cell death but not the cells with BAK. BAM7 could be developed to a new generation of apoptotic modulators that directly activate BCL-2 family executioner proteins in cancer

and other diseases driven by pathologic apoptotic blockades [1].

References:
[1] Evripidis Gavathiotis, Denis E Reyna, Joseph A Bellairs, Elizaveta S Leshchiner, and Loren D Walensky. Direct and selective small-molecule activation of proapoptotic BAX. Nat Chem Biol. 2012 July ; 8(7): 639–645.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt405.47
Cas No.331244-89-4
FormulaC21H19N5O2S
SynonymsBAM 7;BAM-7
SolubilityLimited solubility, soluble in DMSO
Chemical Name(4E)-4-[(2-ethoxyphenyl)hydrazinylidene]-5-methyl-2-(4-phenyl-1,3-thiazol-2-yl)pyrazol-3-one
SDFDownload SDF
Canonical SMILESCCOC1=CC=CC=C1NN=C2C(=NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

MEF cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM, 20 μM, 30 μM and 40 μM

Applications

Co-incubation of BAM7 (10 μM, 20 μM, 30 μM and 40 μM) and monomeric BAX (5 μM) induced dose- and time-responsive BAX oligomerization. BAM7 selectively impaired the viability of Bak-/- MEFs but had no effect on MEFs that lack BAX (Bax-/-) or both BAX and BAK (Bax-/- Bak-/-). BAM7 dose-dependently impaired the viability of BAX-reconstituted, but not BAXK21E-reconstituted, Bax-/- Bak-/- MEFs. Bak-/- MEFs demonstrated the morphologic features of apoptosis in response to BAM7 treatment (15 μM).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Gavathiotis E, Reyna D E, Bellairs J A, et al. Direct and selective small-molecule activation of proapoptotic BAX[J]. Nature chemical biology, 2012, 8(7): 639-645.

Biological Activity

Description BAM7 is a direct and selective activator of BAX with IC50 value of 3.3 μM.
Targets BAX          
IC50 3.3 μM          

Quality Control

Quality Control & MSDS

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Chemical structure

BAM7