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抑制剂/激活剂

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凋亡与自噬

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MG-132 Z-Leu-Leu-Leu-al; MG132

MG132 ((S,R,S)-(-)-MG-132, Z-Leu-D-Leu-Leu-al)是一种有效的蛋白酶体(ChTL, TL和PGPH)抑制剂。MG132对calpain也有抑制作用(IC50=1.2 μM)。MG-132可用于诱导帕金森病动物疾病模型。

货号：
TK0114
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	133407-82-6
生物活性	MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
分子式	C26H41N3O5
分子量	475.62
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : 100 mg/mL (210.25 mM; Need ultrasonic)
体内研究	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).
体外研究	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.
纯度及产品资料	98%

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