MG-132

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MG-132 (Z-Leu-leu-leu-al, Zlllal) 是一种有效、可逆、细胞可渗透的蛋白酶体抑制剂，抑制蛋白酶体和钙蛋白酶的 IC50 分别为 0.1 和 1.2 μM。

MG-132 (Z-Leu-leu-leu-al, Zlllal) is a potent, reversible, and cell-permeable proteasome inhibitor with IC50 of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively; induces neurite outgrowth in PC12 cells with optimal concentrations of 20 nM, inhibits autolytic activation of calpain in rabbit erythrocytes at 100 uM; demonstrates in vivo antitumor activity.(In Vitro):MG-132 (Z-Leu-Leu-Leu-al) initiates neurite outgrowth in PC12 cells at a low concentration (30 nM) and is a very strong inhibitor of 20S proteasome.MG-132 (10 μM; 1 hour) reverses the effects of TNF- α on I κ B degradation and NF-κ B activation in A549 cells.MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition.MG-132 (10-40 μM; 24 hours) significantly reduces the viability of C6 glioma cells in both time- and concentration-dependent manners and shows the IC50 of 18.5 μM at 24 hours.MG-132 (18.5 μM; 24 hours) induces down-regulation of anti-apoptotic proteins Bcl-2 and XIAP and up-regulates expression of pro-apoptotic protein Bax and caspase-3.(In Vivo):MG132 (10 mg/kg; i.p.; daily for 25 days starting 5 days after EC9706 cells injection) significantly inhibits tumor growth of the EC9706 xenograft without causing toxicity to mice.MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors.MG-132 (1-10 μg/kg/24 hours; subcutaneously implanted osmotic pumps; for 8 days) greatly increases the expression levels of β-dystroglycan, α-dystroglycan, α-sarcoglycan, and dystrophin in skeletal muscle lysates in mice (six-month-old male C57BL/10ScSn DMD mdx mice).

Cell Viability Assay Cell Line:C6 glioma cellsConcentration:10, 20, 30, 40 μM Incubation Time:24 hours Result:Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC50 of 18.5 μM at 24 hours.Western Blot AnalysisCell Line:A549 cells Concentration:10 μM Incubation Time:1 hour Result:Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.

Animal Model:5- to 6-weeks old female athymic nude mice (EC9706 xenograft)Dosage:10 mg/kg Administration:I.p.; daily for 25 days starting 5 days after EC9706 cells injection Result:Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.Animal Model:Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells)Dosage:1 mg/kg Administration:Intravenous injection; twice a week for 4 weeks Result:The growth inhibition rates in HeLa tumors was 49% compared to the control.

MG132 | MG 132

Proteasome/Ubiquitin

Proteasome

Proteasome

Cancer

——

133407-82-6

475.6

C26H41N3O5

>98% (HPLC)

10 mM in DMSO

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

L-Leucinamide, N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-

(-20℃)

With Ice Pack

≥ 2 years