research use only
Cat.No.S7105
| Related Targets | Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas |
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| Other Bcl-2 Inhibitors | Navitoclax (ABT-263) S63845 ABT-737 Obatoclax Mesylate (GX15-070) A-1331852 A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77 |
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In vitro |
DMSO
: 2 mg/mL
(4.93 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Working concentration: mg/ml;
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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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| Molecular Weight | 405.47 | Formula | C21H19N5O2S |
Storage (From the date of receipt) | |
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| CAS No. | 331244-89-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CCOC1=CC=CC=C1N=NC2=C(NN(C2=O)C3=NC(=CS3)C4=CC=CC=C4)C | ||
| Features |
Does not interact with the BH3-binding pocket of antiapoptotic proteins or proapoptotic BAK and induces cell death in a BAX-dependent fashion.
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| Targets/IC50/Ki |
Bax
3.3 μM
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| 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.
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| Kinase Assay |
Fluorescence polarization binding assays
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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.
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References |
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