BH3I1 是一种BCL-2家族拮抗剂，作用于p53/Mdm2，Kd为 5.3 μM。它抑制BakBH3 肽与BCL-xL结合，Ki为 2.6 μM。

BH3I-1 is a Bcl-2 antagonist.

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].

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)

300817-68-9

C15H14BrNO3S2

400.31

BHI1

H2O:<1 mgml
Ethanol:11 mg/mL (27.5 mM)
DMSO:60 mg/mL (149.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years