BH3I-1 inhibits Bcl-xL heterodimerization in vitro. It also induces cytochrome c release. 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.
|Cell lines||Jurkat cells|
|Preparation method||Cells (5×10^4 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.|
|Concentrations||30 or 90 μM|
|Incubation time||48 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||64 mg/mL in DMSO|
Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2.
Porter JR, et al. Chem Commun (Camb). 2010 Nov 14;46(42). PMID: 20856941.
Enhancement of radiation sensitivity with BH3I-1 in non-small cell lung cancer.
Roa W, et al. Clin Invest Med. 2005 Apr;28(2):55-63. PMID: 15909480.
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