BH3I-1

BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.

BH3I-1 Chemical Structure

BH3I-1 Chemical Structure

CAS No. 300817-68-9

Purity & Quality Control

Batch: S817701 DMSO]64 mg/mL]false]Ethanol]13 mg/mL]false]Water]Insoluble]false Purity: 99.08%
99.08

BH3I-1 Related Products

Signaling Pathway

Biological Activity

Description BH3I-1 is a Bcl-XL-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.
Targets
BH3-Bcl-xL interaction [1] p53/MDM2 [2]
2.4 μM(Ki) 5.3 μM(Kd)
In vitro
In vitro BH3I-1 inhibits Bcl-xL heterodimerization in vitro. It also induces cytochrome c release[1]. BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1a interactions[2].
Cell Research Cell lines Jurkat cells
Concentrations 30 or 90 μM
Incubation Time 48 h
Method Cells (5×104 cells per well) are seeded into white 96-well plates (Costar) and treated with various concentrations of the compounds for 48 h. For zVAD-FMK protection experiments, cells are preincubated with 100 µM zVAD-FMK for 1 h before the addition of chemicals. Cell viability is determined with an MTS assay. For PI staining experiments, cells are grown in 24-well plates and then incubated with 2 µg ml/L PI. Cell death is determined by FACS analysis.

Chemical Information & Solubility

Molecular Weight 400.31 Formula

C15H14BrNO3S2

CAS No. 300817-68-9 SDF Download BH3I-1 SDF
Smiles CC(C)C(C(=O)O)N1C(=O)C(=CC2=CC=C(C=C2)Br)SC1=S
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (159.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.
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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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