BH3I-1

Catalog No.S8177

BH3I-1 Chemical Structure

Molecular Weight(MW): 400.31

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.

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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

Cell Research:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL warmed (159.87 mM)
Ethanol 13 mg/mL warmed (32.47 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 400.31
Formula

C15H14BrNO3S2

CAS No. 300817-68-9
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID