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首页 / 抑制剂/激动剂 / 泛素 / 蛋白酶体 / (R)-MG-132

(R)-MG-132 {[allProObj[0].p_purity_real_show]}

货号：A541748 同义名： (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al

(R)-MG-132可以作为蛋白酶体抑制剂，用于泛素化实验。

(R)-MG-132 化学结构 CAS号：1211877-36-9
(R)-MG-132 化学结构
CAS号：1211877-36-9
(R)-MG-132 3D分子结构
CAS号：1211877-36-9
(R)-MG-132 化学结构 CAS号：1211877-36-9
(R)-MG-132 3D分子结构 CAS号：1211877-36-9
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(R)-MG-132 纯度/质量文件 产品仅供科研

货号：A541748 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome LMP7, IC50: 82 nM

20S proteasome β5, IC50: 36 nM

 		99%+
Epoxomicin ✔ 95%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Trypsin-like proteasomes, IC50: 1 nM

Chymotrypsin-like proteasomes, IC50: 3 μM

 		99%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98% (NMR）
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(R)-MG-132 生物活性

靶点

  • Proteasome

    Proteasome, IC50:100 nM
描述 (R)-MG132 can act as an inhibitor of proteasome and be used in ubiquitination assay.

(R)-MG-132 细胞实验

Cell Line
Concentration Treated Time Description References
mouse brain synaptosomes 10 µM 30 min To investigate the effects of proteasome inhibition on presynaptic architecture and function, results showed that MG132 treatment significantly reversed the structural defects in RIM1α KO synapses and restored release probability to WT levels. J Cell Biol. 2013 May 27;201(5):725-40.
HEI-193 schwannoma cells 2.5 μM 24, 48, 72 h To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the proliferation of schwannoma cells. Results showed that MG-132 enhanced the inhibitory effect of Nutlin-3 on cell proliferation. EBioMedicine. 2018 Oct;36:252-265.
RT4-D6P2T schwannoma cells 2.5 μM 24, 48, 72 h To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the proliferation of schwannoma cells. Results showed that MG-132 enhanced the inhibitory effect of Nutlin-3 on cell proliferation and narrowed the sensitivity differences between cells with different merlin expression status. EBioMedicine. 2018 Oct;36:252-265.
Naïve CD4+ T cells 10 µM 2 h Promote CD69+ iTregs differentiation Theranostics. 2023 Mar 21;13(6):1892-1905.
RVSMCs 10 μM 6 days Treatment with MG132 or lactacystin halved Pi-induced calcium deposition, demonstrating proteasome inhibition alleviates vascular calcification Nat Commun. 2016 Feb 1;7:10492.
A10 cells (RVSMC line) 10 μM 4 h MG132 treatment enhanced HDAC1 ubiquitination under Pi stimulation, confirming HDAC1 degradation via the proteasomal pathway Nat Commun. 2016 Feb 1;7:10492.
rat vascular smooth muscle cells (RVSMCs) 10 μM 4 h MG132 markedly attenuated Pi-induced HDAC1 reduction, indicating proteasomal inhibition prevents HDAC1 degradation Nat Commun. 2016 Feb 1;7:10492.
Plasmodium falciparum 3D7 parasite-infected red blood cells 100 nM 72 h Inhibition of 26S proteasome activity significantly inhibited α-spectrin degradation and parasite proliferation mBio. 2024 Apr 10;15(4):e0351023.

(R)-MG-132 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice RT4-D6P2T and HEI-193 schwannoma xenograft models Intraperitoneal injection 5 mg/kg Once daily for 14 days To evaluate the inhibitory effect of MG-132 combined with Nutlin-3 on the growth of schwannoma xenografts. Results showed that the combined treatment significantly inhibited tumor growth and induced apoptosis of tumor cells. EBioMedicine. 2018 Oct;36:252-265.
Mice DSS-induced colitis model Intraperitoneal injection 15 μM/kg 9 days Promote CD69+ Tregs differentiation but fail to effectively alleviate colitis Theranostics. 2023 Mar 21;13(6):1892-1905.
Mice VD3-induced vascular calcification model Intraperitoneal injection 2.5 mg/kg Daily administration for 9 days MG132 significantly reduced VD3-induced aortic calcium deposition and prevented HDAC1 downregulation Nat Commun. 2016 Feb 1;7:10492.
Mouse P23H mice Intraperitoneal injection 5 mg/kg Single injection To enhance the detection of ubiquitinated proteins Cell Death Dis. 2019 Jul 18;10(8):547
C57BL/6 mice Plasmodium berghei ANKA infection model Intraperitoneal injection 1.5 mg/kg Once daily for 9 days Inhibition of 26S proteasome activity significantly reduced parasitemia mBio. 2024 Apr 10;15(4):e0351023.
Mice Vitamin D receptor knockout mice Intraperitoneal injection 2.5 mg/kg Once daily for 2 days To assess protein ubiquitination levels, results showed higher total ubiquitination and K48-linked ubiquitination in skeletal muscles of vdr /C0//C0 mice. J Cachexia Sarcopenia Muscle. 2022 Feb;13(1):467-480
Mice Healthy mice Intraperitoneal injection 10 μg/kg Single injection, samples collected after 24 hours MG-132, as a proteasome inhibitor, was used to study the effect of agmatine on β-catenin stability. Results showed that agmatine increased β-catenin stability by suppressing Rnf128-mediated ubiquitination degradation. Gut Microbes. 2024 Jan-Dec;16(1):2348441
Mice Wildtype mice Intraperitoneal injection 50µg/g Single injection, analyzed after 3 hours MG132 significantly increased VEGF receptor levels in type H vessel columns Nat Cell Biol. 2017 Mar;19(3):189-201

(R)-MG-132 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL

(R)-MG-132 技术信息

CAS号1211877-36-9
分子式C26H41N3O5
分子量 475.62
SMILES Code [C@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)CC(C)C)=O)(C(N[C@@H](CC(C)C)C=O)=O)CC(C)C
MDL No. MFCD28580122
别名 (S,R,S)-(-)-MG-132; Z-Leu-D-Leu-Leu-al; MG132
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(220.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

Tags: (R)-MG-132 | 1211877-36-9 | (S,R,S)-(-)-MG-132 | Z-Leu-D-Leu-Leu-al | Proteasome Inhibitor | Metabolic Enzyme/Protease | Proteasome | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | (R)-MG-132 纯度/质量文件 | (R)-MG-132 亚型比较 | (R)-MG-132 生物活性 | (R)-MG-132 实验方案 | (R)-MG-132 技术信息

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