MCI826

MCI826 is a P-glycoprotein (P-gp) antagonist.

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

Research Areas >> Cancer

P-glycoprotein[1]

Verapamil and cyclosporine A, first-generation modulators, and MCI826 (VX-710), a third generation P-gp modulator, are effective enhancers of C6-ceramide response in cells. Verapamil and MCI826 demonstrate weak cytotoxicity alone; however, when administered with C6-ceramide, which is only moderately cytotoxic, viability fell precipitously[1].

Cells are seeded in 96-well plates. Drugs (including MCI826 (VX-710)) are diluted freshly into culture medium containing 1% FBS and added to wells to a total volume of 0.2 mL, thus the final concentration of FBS during treatment is 5.5%. After addition of agents, cells are incubated at 37°C for 72 or 96 hr, and cell viability is determined using cell proliferation assay kit[1].

[1]. Morad SA, et al. Tamoxifen magnifies therapeutic impact of ceramide in human colorectal cancer cells independent of p53. Biochem Pharmacol. 2013 Apr 15;85(8):1057-65.

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