KB-R7943 (mesylate)

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCXrev) with IC50 of 5.7±2.1 μM. KB-R7943 mesylate induces cancer cell death via activating the JNK pathway and blocking autophagic flux.

Product Specifications

CAS Number

[182004-65-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Na+/Ca2+ Exchanger

Type

Reference compound

Related Pathways

Autophagy; Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/KB-R7943-mesylate.html

Concentration

10mM

Purity

99.16

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NC(SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1)=N.CS(=O)(O)=O

Molecular Formula

C17H21N3O6S2

Molecular Weight

427.50

Precautions

H302, H315, H319, H335

References & Citations

[1]Brustovetsky T, et al. KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br J Pharmacol. 2011 Jan;162 (1) :255-70.|[2]Barrientos G, et al. The Na+/Ca2+ exchange inhibitor 2- (2- (4- (4-nitrobenzyloxy) phenyl) ethyl) isothiourea methanesulfonate (KB-R7943) also blocks ryanodine receptors type 1 (RyR1) and type 2 (RyR2) channels. Mol Pharmacol. 2009 Sep;76 (3) :560-8.|[3]Cheng H, et al. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol. 2012 Apr;165 (7) :2260-73.|[4]Long Z, et al. The reverse-mode NCX1 activity inhibitor KB-R7943 promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. Oncotarget. 2016;7 (27) :42059-70.