BAI1

Catalog No.S8865

For research use only.

BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.

BAI1 Chemical Structure

CAS No. 335165-68-9

Selleck's BAI1 has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.
Targets
Bax [1]
(Cell-free assay)
15.0 μM(Kd)
In vitro

BAX activation inhibitor 1 (BAI1) demonstrates inhibition of tBID-induced BAX-mediated membrane permeabilization in a dose dependent manner with an IC50 of 3.3 μM. BAI1 binds to monomeric BAX at a novel allosteric site. BAI1 is a potent inhibitor of BAX conformational activation and oligomerization in solution, not by direct competition with the activator, but rather through an allosteric mechanism that favors the inactive BAX. Moreover, BAI1 inhibited BAX membrane association and translocation induced either by tBID (IC50 = 5 ± 1 μΜ) or BIM SAHB (IC50 = 2 ± 1 μΜ) in a dose dependent manner and with a similar IC50 to BAX-mediated liposomal release. BAI1 selectively inhibits BAX-dependent cell death[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MEFs
  • Concentrations: 0-10 μM
  • Incubation Time: 8 h
  • Method:

    Caspase 3/7 assay of WT MEFs upon pro-apoptotic TNFα/CHX treatment in the absence or presence of co-treatment with BAI1 at indicated doses for 8 hours.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 467.20
Formula

C19H21Br2N3O

CAS No. 335165-68-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1)CC(CN2C3=C(C=C(C=C3)Br)C4=C2C=CC(=C4)Br)O.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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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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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05477862 Not yet recruiting Behavioral: Clinically Designed Improvisatory Music Alzheimer Disease Northwestern University August 15 2022 Early Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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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