KB-R7943 mesylate

Catalog No.S4643 Batch:S464301

Technical Data

Formula	C₁₇H₂₁N₃O₆S₂
Molecular Weight	427.5	CAS No.	182004-65-5
Solubility (25°C)*	In vitro	DMSO	86 mg/mL (201.16 mM)
		Water	Insoluble
		Ethanol	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.)

Preparing Stock Solutions

Biological Activity

Description

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.

Targets

NCX(rev) ^[1]
(Cell-free assay)

5.7 μM

In vitro

KB-R7943 inhibits the reverse NCX more potently than its forward mode, thus occludes NCX-mediated Ca2+ extrusion and elevates intracellular Ca²⁺ level of melanoma.^[3]

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines Flua-4 AM loaded A2058 melanoma cells Concentrations 25 or 50 µM Incubation Time 5 min Method Cells were plated in 96-well cell culture plates at 6000 per well and cultured overnight. Cells were treated with test reagents for 24–72 h according to different requirements. Cells were cultured in 96-well plates at 6000 per well and loaded with the cell membrane permeable Ca²⁺ dye Fluo-4 AM (5 μM) in HEPES-buffered solution for 40 min. The HEPES solution was supplemented with 1% FBS at pH 7.4.

Cell Assay:^{^[3]}

Cell lines
Flua-4 AM loaded A2058 melanoma cells
Concentrations
25 or 50 µM
Incubation Time
5 min
Method
Cells were plated in 96-well cell culture plates at 6000 per well and cultured overnight. Cells were treated with test reagents for 24–72 h according to different requirements. Cells were cultured in 96-well plates at 6000 per well and loaded with the cell membrane permeable Ca²⁺ dye Fluo-4 AM (5 μM) in HEPES-buffered solution for 40 min. The HEPES solution was supplemented with 1% FBS at pH 7.4.

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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