MG-262

MG-262 (Z-Leu-Leu-LeuB(OH)2; ZL3B) is a reversible proteasome inhibitor. MG-262 down-regulates VEGF receptor Flt-1. MG-262 inhibits cell growth and induces apoptosis in malignant cells. MG-262 induces reactive oxygen species (ROS). MG-262 can be used for anti-cancer study^{[1][2][3][4][5]}. In Vitro:MG-262 (1 μM, 16 h) down-regulates the gene expression of the VEGF receptor Flt-1 (vascular endothelial growth factor receptor 1) in explant cultures of the developing chicken pecten oculi^[1].
MG-262 (500 nM, 12 h) prevents the induction of Flt-1 by Lipopolysaccharide (LPS) (HY-D1056) in macrophages and down-regulates the expression of Flt-1 after LPS induction^[1].
MG-262 (500 nM, 12 h) down-regulates Flt-1 gene expression in cultures of human microvascular endothelial cells^[1].
MG-262 (0.1 nM-1 μM, 24 h) can concentration-dependently increase IL-8 promoter and activator protein-1 (AP-1) activities, but inhibits NF-κB activation (IC₅₀ = 1-3 nM) induced by cytokines in HEK293 cells^[2].
MG-262 (0.1 μM, 5-180 min) increases intracellular ROS in time-dependent manner in HEK293 cells^[2].
MG262 (0.125-1 μM, 48 h) inhibits the growth of H22 and K562 cells, and has synergistic effect combined with Gambogic Acid (GA) (HY-N0087)^[3].
MG262 (0.025 μM, 24 h) induces apoptotic cell death when combined with GA in H22 and K562 cells^[3].
MG262 (0.025 μM, 12 or 24 h) induces cleavage of PARP as well as cleavage/activation of caspases 8 and 9 when combined with GA, but not when used alone in K562 cells ^[3].
In Vivo:MG-262 (5 μmol/kg (2.5 mg/kg); i.v.; 20 hours before collecting tissue samples) accumulates GFPdgn protein^[4].
MG-262 (1-5 μmol/kg (0.5-2.5 mg/kg); i.p.; 20 h before the test) accumulates the GFP reporter in the liver, indicating substantial impairment of the ubiquitin/proteasome system in Ub^G76V-GFP/1 mice^[5].