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BH3I-1

Cat. No. M5266
BH3I-1 Structure
Synonym:

BHI1; BH 3I1

Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 110  USD110 In stock
25mg USD 220  USD220 In stock
50mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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
Animal models
Formulation
Dosages
Administration
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Porter JR, et al. Chem Commun (Camb). Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2.

[2] Roa W, et al. Clin Invest Med. Enhancement of radiation sensitivity with BH3I-1 in non-small cell lung cancer.

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  Catalog
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Keywords: BH3I-1, BHI1; BH 3I1 supplier, Bcl-2, inhibitors, activators


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