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Mz325 is a dual inhibitor of histone deacetylase 6 (HDAC6) and sirtuin 2 (SIRT2; IC50s = 0.043 and 0.32 µM, respectively, in a cell-free assay).1 Mz325 is a heterobifunctional molecule that contains an HDAC6 inhibitor conjugated to a SIRT2 inhibitor via a triazole linker. It is selective for HDAC6 and SIRT2 over HDAC1, -2, and -3 (IC50s = 2.2, 6, and 2.5 µM, respectively) and SIRT1 and -3 (IC50s = >100 µM for both). Mz325 increases α-tubulin acetylation in PC-3M-luc prostate cancer cells and inhibits growth in HGC-27 gastric cancer, W1 ovarian cancer, MCF-7 breast cancer, and PC-3M-luc cells (EC50s = 12.9, 19.2, 21.1, and 30.1 µM, respectively).
WARNING This product is not for human or veterinary use.
1. Development of first-