MG-132 (Z-Leu-Leu-Leu-al) 是一种有效的，可逆的蛋白酶体 (proteasome) 抑制剂，IC50为 100 nM。MG-132 有效阻断 26S 蛋白酶体复合物的蛋白水解活性。MG-132 是一种肽醛，是自噬 (autophagy) 激活剂。MG-132 还诱导凋亡 (apoptosis)。
| 生物活性 | MG-132 (Z-Leu-Leu-Leu-al) is a potentproteasomeandcalpaininhibitor withIC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26Sproteasomecomplex. MG-132, a peptide aldehyde, also is anautophagyactivator. MG-132 also inducesapoptosis[1][2][3]. |
| IC50& Target | IC50: 100 nM (Proteasome), 1.2 μM (Calpain)[1][3] |
体外研究
(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[3].
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[4].
MG-132 (0.75-5 μM; 24 hours) potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition[5].
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 IC50of 18.5 μM at 24 hours[6].
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[6].
Cell Viability Assay[3] | 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 IC50of 18.5 μM at 24 hours. |
Western Blot Analysis[3] | 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. |
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体内研究
(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[7].
MG-132 (1 mg/kg; i.v.; twice a week for 4 weeks) shows potent tumor inhibitory effect against mice bearing HeLa tumors[8].
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)[9].
| 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)[8] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(210.25 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1025 mL | 10.5126 mL | 21.0252 mL | | 5 mM | 0.4205 mL | 2.1025 mL | 4.2050 mL | | 10 mM | 0.2103 mL | 1.0513 mL | 2.1025 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.67 mg/mL (3.51 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (3.51 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 1.67 mg/mL (3.51 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (3.51 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.67 mg/mL (3.51 mM); Clear solution
此方案可获得 ≥ 1.67 mg/mL (3.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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