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Calpain Inhibitor I, ALLN Catalog No.GC12527

Calpain I/II/ B/L inhibitor

Size Price Stock Qty
10mM (in 1mL DMSO)
$58.00
In stock
5mg
$37.00
In stock
25mg
$113.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Cell experiment [1]:

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 experiment [2]:

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.

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.

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Chemical Properties

Cas No. 110044-82-1 SDF
Synonyms Ac-LLnL-CHO, MG-101, MG101,N-Acetyl-L-leucyl-L-leucyl-L-norleucinal, N-Acetyl-Leu-Leu-Nle-al,Calpain Inhibitor I
Chemical Name 2-acetamido-4-methyl-N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]pentanamide
Canonical SMILES CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C
Formula C20H37N3O4 M.Wt 383.54
Solubility ≥19.1mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.