1. Membrane Transporter/Ion Channel Autophagy
  2. Na+/Ca2+ Exchanger Autophagy
  3. KB-R7943 mesylate

KB-R7943 mesylate 

Cat. No.: HY-15415 Purity: 99.16%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

KB-R7943 mesylate Chemical Structure

KB-R7943 mesylate Chemical Structure

CAS No. : 182004-65-5

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

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Description

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.

IC50 & Target

IC50: 5.7±2.1 µM (Na+/Ca2+ exchanger)[1]

In Vitro

KB-R7943 mesylate blocks NMDAR-mediated ion currents, and inhibits NMDA-induced increase in cytosolic Ca2+ with IC50=13.4±3.6 µM but accelerates calcium deregulation and mitochondrial depolarization in glutamate-treated neurons. KB-R7943 depolarizes mitochondria in a Ca2+-independent manner. KB-R7943 inhibits 2,4-dinitrophenol-stimulated respiration of cultured neurons with IC50=11.4±2.4 µM. In addition to NCXrev, KB-R7943 dose-dependently and reversibly blocked ion currents elicited by NMDA. KB-R7943 dose-dependently inhibits NMDA-induced increases in [Ca2+]c with IC50=13.4±3.6 µM confirming the inhibition of NMDA receptors observed in electrophysiological experiments[1]. wtRyR1-HEK 293 pretreated with KB-R7943 (10 μM, 10 min) dissolved in the bulk perfusion exhibited significantly attenuated responses to caffeine. In this regard, KB-R7943 produced more pronounced inhibition of caffeine-induced Ca2+ release elicited by 1 mM compared with 0.5 and 0.75 mM (60 versus 58 versus 37%, p<0.05, respectively)[2]. KB-R7943 inhibits both IhERG and native IKr rapidly on membrane depolarization with IC50 values of ~89 and ~120 nM, respectively, for current tails at −40 mV following depolarizing voltage commands to +20 mV. IhERG inhibition by KB-R7943 exhibits both time- and voltage-dependence but shows no preference for inactivated over activated channels[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

427.50

Formula

C17H21N3O6S2

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (233.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.16%

References
Cell Assay
[2]

EK 293 cells stably expressing the wtRyR1 (wtRyR1-HEK 293) are maintained in Dulbecco's modified Eagle's medium supplemented with 2 mM glutamine, 100 μg/mL streptomycin, 100 U/mL penicillin, 1 mM sodium pyruvate, and 10% fetal bovine serum at 37°C under 5% CO2. wtRyR1-HEK 293 cells are loaded with 5 μM Fluo-4 acetoxymethyl ester at 37°C for 30 min to measure Ca2+ transients in an imaging buffer consisting of 140 mM NaCl, 5 mM KCl, 2 mM MgCl2, 2 mM CaCl2, 10 mM HEPES, and 10 mM glucose, pH 7.4, supplemented with 0.05% bovine serum albumin. The cells are washed three times with imaging buffer and additionally incubated for 20 min at room temperature. Dye-loaded cells are washed three times with imaging buffer and imaged with a charge-coupled device camera with a 40× objective lens attached to an IX-71 microscope. The sequence of images is captured and monitored using EasyRatioPro. Caffeine dissolved in the imaging buffer is focally applied for 15 s using AutoMate Scientific. KB-R7943 is dissolved in the imaging buffer, and wtRyR1-HEK 293 cells are incubated for 10 min before the application of caffeine[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
KB-R7943 mesylate
Cat. No.:
HY-15415
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