NSC 23925

NSC 23925 is a non-substrate inhibitor of P-glycoprotein (P-gp).¹ It selectively reverses multidrug resistance mediated by P-gp over resistance mediated by multidrug resistance-associated protein 1 (MRP1/ABCC1) or breast cancer resistance protein (BCRP/ABCG2). It resensitizes paclitaxel-resistant SKOV3_TR and OVCAR-8_TR cells to paclitaxel (Item No. 10461). NSC 23925 reverses P-gp efflux, increasing the intracellular accumulation of P-gp substrates, including calcein AM (Item No. 14948) in multidrug-resistant SKOV3_TR and OVCAR-8_TR cells. It prevents paclitaxel-induced overexpression of the P-gp gene MDR1 and P-gp protein level increases in OVCAR-8 cells.² It also prevents the development of paclitaxel-induced multidrug resistance in a SKOV3 mouse xenograft model when administered at a dose of 50 mg/kg per day in combination with paclitaxel.

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1. Duan, Z., Choy, E., and Hornicek, F.J. NSC23925, identified in a high-throughput cell-based screen, reverses multidrug resistance. PLoS One 4(10), e7415 (2009).

2. Yang, X., Feng, Y., Gao, Y., et al. NSC23925 prevents the emergence of multidrug resistance in ovarian cancer in vitro and in vivo. Gynecol. Oncol. 137(1), 134-142 (2015).