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VGSC blocker-1

Catalog No. T39717   CAS 2230472-55-4

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.

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VGSC blocker-1 Chemical Structure
VGSC blocker-1, CAS 2230472-55-4
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Biological Description
Chemical Properties
Storage & Solubility Information
Description VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.
In vitro VGSC blocker 1 (compound 1), at concentrations ranging from 1.0 to 10 μM, effectively inhibits the human breast cancer cell line MDA-MB-231[1]. Specifically, this compound reduces cell viability and impacts cell invasion within this cell line. Experimental results demonstrate that VGSC blocker 1 decreases INa peak currents by 34.9% at a concentration of 1 µM, alongside a marginal 0.3% inhibition of cell invasion at the same concentration. These effects surpass the efficacy thresholds previously established at 0.1 µM for significant nNav1.5 current blockade and 1 µM for cell invasion inhibition, underscoring the compound's potent biological activity against MDA-MB-231 cells.
Molecular Weight 386.531
Formula C24H32F2N2
CAS No. 2230472-55-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Dutta S, et al. Discovery and evaluation of nNav1.5 sodium channel blockers with potent cell invasion inhibitory activity in breast cancer cells. Bioorg Med Chem. 2018;26(9):2428-2436.

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Keywords

VGSC blocker-1 2230472-55-4 VGSC blocker 1 VGSC blocker1 inhibitor inhibit

 

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