NSC636795

NSC636795 is an inhibitor of the ABCG2 transporter. NSC636795 inhibits ABCG2-mediated PhA efflux. NSC636795 also partially reverses ABCG2-mediated resistance to Topotecan (HY-13768). NSC636795 can be used in studies related to ABCG2-mediated antitumor drug resistance^[1]. In Vitro:NSC636795 (20 μM; 10 min pre-incubation before IAAP addition) weakly inhibits the binding of [¹²⁵I]IAAP to ABCG2 in crude membranes of MCF-7 FLV1000 cells, with an observed inhibition rate of 15%^[1].
NSC636795 (10 μM; 30 min PhA incubation followed by 1 h efflux incubation) inhibits ABCG2-mediated PhA efflux in HEK 293 cells transfected with wild-type ABCG2, as evidenced by a 2.4-fold increase in intracellular PhA fluorescence intensity^[1].
NSC636795 (10 μM; 96 h) partially reverses ABCG2-mediated topotecan resistance in HEK 293 cells transfected with wild-type ABCG2, reducing the relative resistance value from 19 to 4.9^[1].
The combination of NSC636795 (10 μM; 96 h) with Topotecan partially reverses ABCG2-mediated Topotecan resistance in ABCG2-transfected HEK293 cells, reducing the relative resistance fold from 19 to 4.9; this concentration of NSC636795 results in less than 10% cell death in both empty vector-transfected and ABCG2-transfected cells^[1].