产品说明书

MG-101

Print
Chemical Structure| 110044-82-1 同义名 : Calpain inhibitor I;ALLN;AcLLnLCHO, Ac-Leu-Leu-Nle-Aldehyde.;Ac-Leu-Leu-Nle-Aldehyde;Calpain inhibitor-1;Ac-LLnL-CHO
CAS号 : 110044-82-1
货号 : A158847
分子式 : C20H37N3O4
纯度 : 98%+
分子量 : 383.526
MDL号 : MFCD00065505
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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
实验方案
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
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.