MG-262  (Synonyms: Z-Leu-Leu-LeuB(OH)2; ZL3B)

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]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

491.43

C₂₅H₄₂BN₃O₆

179324-22-2

Solid

White to off-white

O=C(N[C@H](B(O)O)CC(C)C)[C@H](CC(C)C)NC([C@H](CC(C)C)NC(OCC1=CC=CC=C1)=O)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Mezquita J, et al. Down-regulation of Flt-1 gene expression by the proteasome inhibitor MG262. J Cell Biochem. 2003 Aug 15;89(6):1138-47.  [Content Brief]

  [2]. Wu HM, et al. Proteasome inhibitors stimulate activator protein-1 pathway via reactive oxygen species production. FEBS Lett. 2002 Aug 28;526(1-3):101-5.  [Content Brief]

  [3]. Huang H, et al. Gambogic acid enhances proteasome inhibitor-induced anticancer activity. Cancer Lett. 2011 Feb 28;301(2):221-8.  [Content Brief]

  [4]. Kumarapeli AR, et al A novel transgenic mouse model reveals deregulation of the ubiquitin-proteasome system in the heart by doxorubicin. FASEB J. 2005 Dec;19(14):2051-3.  [Content Brief]

  [5]. Lindsten K, et al. A transgenic mouse model of the ubiquitin/proteasome system. Nat Biotechnol. 2003 Aug;21(8):897-902.  [Content Brief]