Biological Activity
NR-160 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 0.03 μM).1 It is selective for HDAC6 over HDAC1, -2, -3, -4, and -8 (IC50s = 5.18, 2.26, 8.48, 55.4, and 14.7 μM, respectively). NR-160 is cytotoxic against a panel of seven cancer cell lines (IC50s = 22.5-51.8 μM). It enhances cytotoxicity induced by bortezomib in HL-60 cells, as well as cytotoxicity induced by epirubicin or daunorubicin in CCRF-HSB-2 T cell acute lymphoblastic leukemia cells.
References
1.Re?ing, N., S?nnichsen, M., Osko, J.D., et al.Multicomponent synthesis, binding mode, and structure-activity relationship of selective histone deacetylase 6 (HDAC6) inhibitors with bifurcated capping groupsJ. Med. Chem.63(18)10339-10351(2020)
