切换导航

Calpain Inhibitor I, ALLN

现货
Catalog No.
A2602
Calpain I/II/ B/L抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 860.00
现货
5mg
¥ 550.00
现货
25mg
¥ 1,650.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Calpain Inhibitor I is an inhibitor of calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively.

Calpain inhibitor I combined with Ad/gTRAIL induced cell death dramatically in DLD1-TRAIL/R cells, while calpain alone had only minimal killing effects. The combination of calpain inhibitor I and TRAIL protein resulted in cleavage of both caspase-8 and caspase-3 to active subunits [1].

Calpain inhibitor I treated male Sprangue-Dawley rats have seen reductions of P-selectin/ICAM-1 expression, neutrophil infiltration, lipid peroxidation, nitrotyrosine, PAR formation as well as IκB-α degradation [2].

Reference:
[1] Zhu H1, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther. 2004 May;9(5):666-73.
[2] Marzocco S1, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S.  Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44.

文献引用

1. Ednie AR, Parrish AR, et al. "Reduced hybrid/complex N-glycosylation disrupts cardiac electrical signaling and calcium handling in a model of dilated cardiomyopathy." J Mol Cell Cardiol. 2019 Jul;132:13-23. PMID:31071333
2. YU HUANG. "STUDY OF REGULATED CELL DEATH IN TWO SYSTEMS: PD-1 IN NATURAL KILLER CELLS AND RIP3 IN NEURONS."The University of Texas. 2018.
3. KoraMagazi A, Wang D, et al. "Rhein triggers apoptosis via induction of endoplasmic reticulum stress, caspase-4 and intracellular calcium inprimary human hepatic HL-7702 cells." Biochem Biophys Res Commun. 2016 Apr 22;473(1):230-236. PMID:27003256

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt383.54
Cas No.110044-82-1
FormulaC20H37N3O4
SynonymsAc-LLnL-CHO, MG-101, MG101,N-Acetyl-L-leucyl-L-leucyl-L-norleucinal, N-Acetyl-Leu-Leu-Nle-al,Calpain Inhibitor I
Solubility≥19.1mg/mL in DMSO
Chemical Name2-acetamido-4-methyl-N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]pentanamide
SDFDownload SDF
Canonical SMILESCCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

DLD1-TRAIL/R细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

0、10、20和50 μM;96小时

实验结果

在DLD1-TRAIL/R细胞中,Calpain Inhibitor I和Ad/gTRAIL联合用药显著诱导细胞死亡。当单独使用Calpain Inhibitor I和Ad/gTRAIL时,两者的作用最小。

动物实验 [2]:

动物模型

内脏动脉阻断性(SAO)休克大鼠

给药剂量

15 mg/kg;腹腔注射

实验结果

在再灌注前,先腹腔注射15 mg/kg Calpain Inhibitor I可以显著减少IκB-α降解、再灌注回肠中的P-选择素/ICAM-1强度,中性粒细胞浸润以及丙二醛水平。同时,Calpain Inhibitor I预处理显着改善平均动脉血压和再灌注组织的组织学状态。

其他注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Zhu H1, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther.?2004 May;9(5):666-73.

[2]. Marzocco S1, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S. Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44.

生物活性

描述 Calpain Inhibitor I,ALLN是calpain I、calpain II、cathepsin B和cathepsin L的抑制剂,Ki值分别为190 nM、220 nM、150 nM和500 pM。
靶点 calpain I calpain II cathepsin B cathepsin L    
IC50 190 nM(Ki) 220 nM(Ki) 150 nM(Ki) 500 nM(Ki)    

质量控制

化学结构

Calpain Inhibitor I, ALLN

相关生物数据

Calpain Inhibitor I, ALLN

相关生物数据

Calpain Inhibitor I, ALLN

相关生物数据

Calpain Inhibitor I, ALLN

相关生物数据

Calpain Inhibitor I, ALLN