MRS8431

MRS8431 (0.1-25 μM; 20 min) potently inhibits ABCG2-mediated ATPase activity in High-Five insect cell membranes with an IC₅₀ of 0.16 μM, showing significant inhibition at concentrations of 1 μM and above^[1].
MRS8431 (0.1-25 μM; 20 min) has no significant effect on P-gp-mediated ATPase activity at concentrations up to 1 μM, and only partial inhibitory effects at higher concentrations (10 and 25 μM) in High-Five insect cell membranes^[1].
MRS8431 (0-2.5 μM) potently inhibits ABCG2-mediated transport of mitoxantrone (IC₅₀ 0.50 μM) and pheophorbide A (IC₅₀ 0.88 μM) in ABCG2-expressing HEK293 R-5 cells^[1].
MRS8431 (10 μM) has only a marginal partial inhibitory effect (35.4% at 10 μM) on P-gp-mediated BD-verapamil transport in P-gp-expressing HeLa-S3 cells^[1].
MRS8431 (up to >25 μM; 72 h) is cytotoxic to both HEK293-pcDNA control cells (IC₅₀ 2.20 μM) and ABCG2-expressing HEK293 R-5 cells (IC₅₀ 1.98 μM), and is not transported by ABCG2^[1].
MRS8431 (0.6 μM; 72 h) significantly sensitizes ABCG2-expressing HEK293 R-5 cells to mitoxantrone, reducing mitoxantrone's IC₅₀ and eliminating ABCG2-mediated chemoresistance^[1].

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