BH3I-1

Catalog No.S8177

For research use only.

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

CAS No. 300817-68-9

Purity & Quality Control

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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

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].

Protocol (from reference)

Cell Research:[1]
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 400.31
Formula

C15H14BrNO3S2

CAS No. 300817-68-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C(C(=O)O)N1C(=O)C(=CC2=CC=C(C=C2)Br)SC1=S

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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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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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