BH3I-1

Catalog No.S8177 Batch:S817701

Technical Data

Formula	C₁₅H₁₄BrNO₃S₂
Molecular Weight	400.31	CAS No.	300817-68-9
Solubility (25°C)*	In vitro	DMSO	64 mg/mL (159.87 mM)
		Ethanol	13 mg/mL (32.47 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.

Targets

BH3-Bcl-xL interaction ^[1]	p53/MDM2 ^[2]
2.4 μM(Ki)	5.3 μM(Kd)

In vitro

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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Jurkat cells Concentrations 30 or 90 μM Incubation Time 48 h Method 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.

Cell Assay:^{^[1]}

Cell lines
Jurkat cells
Concentrations
30 or 90 μM
Incubation Time
48 h
Method
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.

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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