VGSC blocker-1

VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability[1].

Research Areas >> Cancer

VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5)[1].

VGSC blocker 1 (1.0 to 10μM) inhibits human breast cancer cell line MDA-MB-231[1]. Cell Viability Assay[1] Cell Line: human breast cancer cell line MDA-MB-231 Concentration: 1.0 to 10μM Incubation Time: 24 hours Result: VGSC blocker 1 blocks INa peak currents 34.9% at 1 uMa and inhibits cell invasion 0.3% at 1 uM. These values are much higher than the concentrations required (0.1 μM and 1 μM) to produce significant nNav1.5 current blockade and cell invasion inhibition.

[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.