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Calpain Inhibitor I,ALLN
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Calpain Inhibitor I,ALLN图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议

产品介绍
Calpain Inhibitor I, ALLN (ALLN) 是一种半胱氨酸蛋白酶抑制剂,可抑制钙蛋白酶 I、钙蛋白酶 II、组织蛋白酶 B 和组织蛋白酶 L,Kis 分别为 190、220、150 和 500 pM。 Calpain Inhibitor I, ALLN 诱导细胞凋亡并抑制肿瘤生长,可用于结肠癌的研究。

Cell lines

DLD1-TRAIL/R cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0, 10, 20 and 50 μM; 96 hrs

Applications

In DLD1-TRAIL/R cells, Calpain Inhibitor I combined with Ad/gTRAIL induced cell death dramatically while Calpain Inhibitor I or Ad/gTRAIL alone only had minimal killing effects.

Animal models

Splanchnic artery occlusion (SAO)-shocked rats

Dosage form

15 mg/kg; i.p.

Applications

Calpain Inhibitor I, given intraperitoneally 30 mins before ischemia at a dose of 15 mg/kg, significantly reduced IκB-α degradation, the intensity of P-selectin/ICAM-1 in the reperfused ileum, neutrophil infiltration as well as malondialdehyde levels. Meanwhile, pretreatment of Calpain Inhibitor I markedly improved mean arterial blood pressure and the histological status of the reperfused tissue.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

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.