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BH3I-1

Cat. No. M5266
BH3I-1 Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 185 In stock
25mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 400.31
Formula C15H14BrNO3S2
CAS Number 300817-68-9
Purity >99%
Solubility 64 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BH3I-1 supplier, Bcl-2, inhibitors

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