产品描述:
SMIP004 is an inhibitor of the E3 ubiquitin ligase S-phase kinase-associated protein 2 (SKP2).{49852} It reduces the levels of SKP2 and induces the accumulation of p27Kip1 and p21Cip21, ubiquitination targets of SKP2, in LNCaP-S14 human prostate cancer cells overexpressing SKP2 when used at a concentration of 40 µM. SMIP004 is cytotoxic to LNCaP-S14 cells (IC50 = 1.09 µM) but not non-cancerous IMR-90 human fibroblasts. It also targets cyclin D1 for proteasomal degradation, as well as induces the unfolded protein response, oxidative stress, apoptosis, and cell cycle arrest at the G1 phase in LNCaP-S14 cells.{49853} SMIP004 (2 mg/kg) reduces immobility time in the forced swim test and tail suspension test, as well as increases the preference for sucrose in the sucrose preference test, in a mouse model of chronic unpredictable stress-induced depression.