产品描述:
SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}