P-gp inhibitor 4

P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells[1].

Research Areas >> Cancer

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

EC50: 94 nM (P-glycoprotein)[1]

P-gp inhibitor 4 (Compound 8b) (0-1 μM, 48 h) significantly increases the cytotoxic effect of antineoplastic drug with co-administration[1]. P-gp inhibitor 4 does not alter the physiological properties of Caco-2 cells barrier model[1]. P-gp inhibitor 4 selectively reduces the activity of P-gp and increases the transport of multiple P-gp substrates across gastro-intestinal barrier[1]. Cell Proliferation Assay[1] Cell Line: MDCK-MDR1 Concentration: 100 nM, 500 nM and 1 μM Incubation Time: 48 h Result: Showed no cytotoxicity. Significantly increased the cytotoxic effect of antineoplastic drug. Cell Viability Assay[1] Cell Line: Caco-2 cells Concentration: 0.1 nM-100 µM Incubation Time: 72 h Result: Displayed a dose-dependence cytotoxicity that was significant at ≥ 10 μM concentration. Did not reduce cell viability at 100 nM.

[1]. Contino M, et al. One molecule two goals: A selective P-glycoprotein modulator increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells. Eur J Med Chem. 2020 Dec 15;208:112843.