BAI1

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

BAI1 Chemical Structure

BAI1 Chemical Structure

CAS No. 335165-68-9

Purity & Quality Control

Batch: S886501 DMSO]18 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.94%
99.94

BAI1 Related Products

Signaling Pathway

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
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].

Cell Research 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.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05477862 Enrolling by invitation
Alzheimer Disease
Northwestern University
October 15 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 467.20 Formula

C19H21Br2N3O

CAS No. 335165-68-9 SDF --
Smiles C1CN(CCN1)CC(CN2C3=C(C=C(C=C3)Br)C4=C2C=CC(=C4)Br)O.Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 18 mg/mL ( (38.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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