MG-101 | Calpain inhibitor I | Cysteine Protease Inhibitor

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钙蛋白酶抑制剂I /MG-101 {[allProObj[0].p_purity_real_show]}

货号：A158847 同义名： Calpain inhibitor I;ALLN

MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM).

MG-101 化学结构
CAS号：110044-82-1

MG-101 3D分子结构
CAS号：110044-82-1

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MG-101 纯度/质量文件产品仅供科研

货号：A158847 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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Cysteine Protease 亚型比较
蛋白酶体亚型比较

产品名称	Cysteine Protease ↓ ↑	纯度
Z-FA-FMK	✔	99%+
Leupeptin hemisulfate	✔	97%
PMSF	✔	95%
PD 151746	+ m-calpain, IC50: 5.33 μM μ-Calpain, IC50: 260 nM	98%
Odanacatib	++++ Cathepsin K (rabbit), IC50: 1 nM Cathepsin K (human), IC50: 0.2 nM	99%+
E-64	+++ Cysteine protease, IC50: 9 nM	99%+
E 64c	✔	95%
E-64d	✔	99%+
MG-101	✔	98%+
Calpeptin	++ Calpain I (porcine erythrocytes), ID50: 52 nM Calpain II (porcine kidney), ID50: 40 nM	98%+
Cathepsin inhibitor 1	+++ Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9	98%
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。

产品名称	20S proteasome ↓ ↑	Proteasome ↓ ↑	纯度
Ixazomib	++++ 20S proteasome, IC50: 3.4 nM 20S proteasome, Ki: 0.93 nM		99%+
Delanzomib	+++ Chymotrypsin-like proteasome, IC50: 3.8 nM		98%
Celastrol	+ 20S proteasome, IC50: 2.5 μM		98%
MLN9708	+++ 20S proteasome, IC50: 3.4 nM 20S proteasome, Ki: 0.93 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	✔		99%
PI-1840	++ Chymotrypsin-like proteasome, IC50: 27 nM		98%
VR23		+++ Chymotrypsin-like proteasomes, IC50: 3 μM Trypsin-like proteasomes, IC50: 1 nM	98%
Carfilzomib		++ Proteasome, IC50: 5 nM	98%
(R)-MG-132		+ Proteasome, IC50: 100 nM	98%
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。

MG-101 生物活性

靶点

Cysteine Protease

描述

Calpain is a calcium-activated protease with exist as an inactive proenzyme in the cytosol. When intracellular calcium level is overloaded, it triggers to convert the proenzyme to its active form. Activated calpain then cleaves xytoplasmiv and nuclear substrates, leading to apoptosis^[3]. In transgenic models, the absence of cathepsin B has been associated with enhanced apoptosis, yet cathepsin B also has been shown to contribute to apoptosis. Cathepsin B is part of a proteolytic pathway identified in xenograft models of human glioma; targeting only cathepsin B in these tumors is less effective than targeting cathepsin B in combination with other proteases or protease receptors^[4]. MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively^[5]. Experiment showed that MG-101 (given at 5, 10, or 20mg/kg i.p. in the pleurisy model or at 5mg/kg i.p. every 48 hours in the arthritis model) exerts potent anti-inflammatory effects in vivo and reduced the staining for nitrotyrosine and poly (ADP-ribose) polymerase^[6].

MG-101 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Effect on cofilin1 expressed in HEK293 cells assessed as effect on cofilin1; Limk2 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay	16680159
HeLa cells		Cytotoxicity assay	48 h	Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTS assay, CC50=25.1 μM	23357632
L1210 cells		Function assay		Inhibitory concentration of the compound was determined against L1210 cells, IC50=3 μM	15634028
melanoma B16 cells		Function assay		Inhibitory concentration of the compound was determined against melanoma B16 cells, IC50=14.5 μM	15634028

MG-101 参考文献

[1]Li SZ, Zhang HH, et al. ALLN hinders HCT116 tumor growth through Bax-dependent apoptosis. Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.

[2]Hiwasa T, Sawada T, et al. Cysteine proteinase inhibitors and ras gene products share the same biological activities including transforming activity toward NIH3T3 mouse fibroblasts and the differentiation-inducing activity toward PC12 rat pheochromocytoma cells. Carcinogenesis. 1990 Jan;11(1):75-80.

[3]Momeni, H. R. Role of calpain in Apoptosis. Cell J. 2011. 13(2), 65-72.

[4]Neha, A. et al. Cathepsin B: multiple roles in cancer. Proteomics Clin Appl. 2014. 8(5-6), 427-37.

[5]Li SZ, et al. ALLN hinders HCT116 tumor growth through Bax-dependent apoptosis. Biochem Biophys Res Commun. 2013. 437(2), 325-330.

[6]Cuzzocrea, S., McDonald, M. C. et al. Calpain Inhibitor I Reduces the Development of Acute and Chronic Inflammation. ELSEVIER. 2000. 157(6), 2065-2079.

MG-101 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.07mL

5.21mL

2.61mL

MG-101 技术信息

CAS号	110044-82-1
分子式	C₂₀H₃₇N₃O₄
分子量	383.526

别名	Calpain inhibitor I;ALLN;AcLLnLCHO, Ac-Leu-Leu-Nle-Aldehyde.;Ac-Leu-Leu-Nle-Aldehyde;Calpain inhibitor-1;Ac-LLnL-CHO
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 120 mg/mL(312.89 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

动物实验配方

钙蛋白酶抑制剂I /MG-101 {[allProObj[0].p_purity_real_show]}

MG-101 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

MG-101 质控信息

MG-101 生物活性

MG-101 细胞研究

MG-101 参考文献

MG-101 实验方案

MG-101 技术信息

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钙蛋白酶抑制剂I /MG-101 {[allProObj[0].p_purity_real_show]}

MG-101 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

MG-101 质控信息

MG-101 生物活性

MG-101 细胞研究

MG-101 参考文献

MG-101 实验方案

MG-101 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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MG-101 纯度/质量文件产品仅供科研