(-)-CXL017

(-)-CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 13.5 uM; selectively suppresses the growth of tumors derived from the MDR cancer cell line, HL60/MX2, in vivo; significantly downregulates Mcl-1 and Bax and up-regulates Noxa, Bim, Bcl-XL, SERCA2, and SERCA3 proteins, along with a reduction in endoplasmic reticulum (ER) calcium content in HL60/MX2 cells; elicits its cytotoxic effect, in part, through inhibition of the SERCA.

References 1. Bleeker NP, et al. Mol Pharm. 2013 Nov 4;10(11):4358-66. View Related Products by Target Other Targets