Mz325

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). 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 alpha-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).. SMILES: CCCCN(CC1=CC=C(C(NO)=O)C=C1)C(CCCCN2C=C(N=N2)COC3=CC=CC(CC4=CN=C(S4)NC(CSC5=NC(C)=CC(C)=N5)=O)=C3)=O. InChi Code: InChI=1S/C38H45N9O5S2/c1-4-5-16-46(22-28-12-14-30(15-13-28)36(50)44-51)35(49)11-6-7-17-47-23-31(43-45-47)24-52-32-10-8-9-29(19-32)20-33-21-39-37(54-33)42-34(48)25-53-38-40-26(2)18-27(3)41-38/h8-10,12-15,18-19,21,23,51H,4-7,11,16-17,20,22,24-25H2,1-3H3,(H,44,50)(H,39,42,48). InChi Key: VNFKTHQLIBPFNF-UHFFFAOYSA-N