Description
InformationInauhzin is a cell-permeableSIRT1inhibitor with an IC50 of 0.7-2 µM and reactivatesp53by inhibiting SIRT1 deacetylation activity.TargetsSIRT1 ; p53In vitroInauhzin (INZ) is a potent p53 activator and mediates p53-dependent cytotoxicity. INZ inhibits cell proliferation by triggering both apoptosis and senescence in p53-containning cells, though it predominantly induces p53-dependent apoptosis. INZ is able to prevent p53 from MDM2-mediated ubiquitylation and proteasomal degradation and protects p53 without either directly inhibiting MDM2 activity towards p53 or interfering with MDMX/MDM2–p53 interaction. INZ induces acetylation of p53, but not tubulin, in cells. Inauhzin is a (sub)micromolar SIRT1i selective over SIRT2/3.In vivoInauhzin (INZ) has good tumour tissue penetration and is able to inhibit tumour growth by inducing p53.Cell Research(from reference)Cell lines：human lung cancer H460, A549, H1299, colon cancer HCT116, HT29, osteosarcoma U2OS and SJSA, breast cancer MCF7, ovarian cancer A2780, IGROV1 and SKOV3 and glioma U87 and U373 cells, as well as human embryonic fibroblast WI-38 and normal human Concentrations：0-10 µM Incubation Time：18 h