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 Experiment | |
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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 |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 400.31 |
Formula | C15H14BrNO3S2 |
CAS Number | 300817-68-9 |
Solubility (25°C) | 60 mg/mL in DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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