Home
Resources
Publications
KB-R7943, a Plasma Membrane Na(+)/Ca(2+) Exchanger Inhibitor, Blocks Opening of the Mitochondrial Permeability Transition Pore

KB-R7943, a Plasma Membrane Na(+)/Ca(2+) Exchanger Inhibitor, Blocks Opening of the Mitochondrial Permeability Transition Pore

Brian M Wiczer, Raluca Marcu, Brian J Hawkins

Biochem Biophys Res Commun. 2014 Jan 31;444(1):44-9.

PMID: 24434143

Abstract:

The isothiourea derivative, KB-R7943, inhibits the reverse-mode of the plasma membrane sodium/calcium exchanger and protects against ischemia/reperfusion injury. The mechanism through which KB-R7943 confers protection, however, remains controversial. Recently, KB-R7943 has been shown to inhibit mitochondrial calcium uptake and matrix overload, which may contribute to its protective effects. While using KB-R7943 for this purpose, we find here no evidence that KB-R7943 directly blocks mitochondrial calcium uptake. Rather, we find that KB-R7943 inhibits opening of the mitochondrial permeability transition pore in permeabilized cells and isolated liver mitochondria. Furthermore, we find that this observation correlates with protection against calcium ionophore-induced mitochondrial membrane potential depolarization and cell death, without detrimental effects to basal mitochondrial membrane potential or complex I-dependent mitochondrial respiration. Our data reveal another mechanism through which KB-R7943 may protect against calcium-induced injury, as well as a novel means to inhibit the mitochondrial permeability transition pore.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
ALP182004644	KB-R7943		182004-64-4 (free base)	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: