133407-82-6
133407-82-6 结构式
基本信息
MG-132
Z-LEU-LEU-LEU-AL
N-[(苄氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-L-亮氨酰胺
Z-LL-CHO
Z-LLL-CHO
(S)-MG132
MG132/MG-132
Z-LEU-LEU-LEU-H
z-leu-leu-leu-al
Z-LEU-LEU-LEU-CHO
Z-LEU-LEU-ALDEHYDE
CALPAIN INHIBITOR IV
物理化学性质
常见问题列表
MG132,蛋白酶体抑制剂是一种有效，可逆，能渗透细细胞的20S蛋白酶抑制剂。它抑制蛋白酶体胰凝乳蛋白酶样肽酶活性的 IC50值为24.2 nM。MG-132以时间和剂量依赖性方式抑制问C6神经胶质瘤细胞增殖（24小时时的IC 50值为18.5μM）。 MG-132通过下调抗细胞凋亡答蛋白Bcl-2和XIAP，促内凋亡蛋白Bax和半胱天冬酶-3的上调以及切割的C端85kDa PARP的产生来诱导细胞凋亡。
MG132通过诱导细胞周期停滞以及引发细胞凋亡来抑制HeLa细胞的生长。 MG-132以时间和剂量依赖性方式抑制C6神经胶质瘤细胞增殖（24小时时的IC 50值为18.5μM）。 MG-132（18.5μM）在3小时时抑制蛋白酶体活性约70％。MG-132通过下调抗细胞凋亡蛋白Bcl-2和XIAP，促凋亡蛋白Bax和半胱天冬酶-3的上调以及切割的C端85kDa PARP的产生来诱导细胞凋亡。 MG-132还会使活性氧增加5倍以上。 孵育48小时后MG-132对HeLa，CaSki和C33A宫颈癌细胞存活率的IC50分别为2.1,3.2和5.2μM。
使用皮下注射检查MG-132对宫颈癌的体内抗肿瘤活性。 异种移植模型。 使用以下方案以1mg / kg注射MG-132：对于携带HeLa肿瘤的小鼠，第1,4,8,12,15,18,23和26天。 与对照相比，MG132的生长抑制率为49％。 MG-132（腹股沟，0.1 mg / kg /天）通过调节ERK1 / 2和JNK1信号通路减轻压力超负荷引起的心脏肥大并改善腹主动脉条带（AAB）大鼠的心脏功能。
IC50: 100 nM (Proteasome), 1.2 μM (Calpain)
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 IC
50
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.
Cell Viability Assay
| Cell Line: | C6 glioma cells |
| Concentration: | 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 IC 50 of 18.5 μM at 24 hours. |
Western Blot Analysis
| Cell 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. |
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).
| 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. |