Calpain Inhibitor XII
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: 19 nM for μ-calpain
Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I.
Calpain is a protein belonging to the family of calcium-dependent, non-lysosomal cysteine proteases expressed ubiquitously in mammals and many other organisms. Calpain inhibitors have been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
In vitro: A series of new dipeptidyl alpha-keto amides of the general structure R1-L-Leu-D,L-AA-CONH-R2 including Calpain Inhibitor XII were synthesized and evaluated as inhibitors for the cysteine proteases calpain I, calpain II, and cathepsin B. Calpain II was more sensitive to these inhibitors Calpain Inhibitor XII than calpain I. Calpain I was also effectively inhibited by Calpain Inhibitor XII, but lower Ki values than with calpain II. Cathepsin B was weakly inhibited by Calpain Inhibitor XII. The best calpain I inhibitor in this study was Calpain Inhibitor XII with Ki value of 19 nM [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Li, Z. ,Ortega-Vilain, A.C.,Patil, G.S., et al. Novel peptidyl α-keto amide inhibitors of calpains and other cysteine proteases. Journal of Medicinal Chemistry 39(20), 4089-4098 (1996).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 482.6 |
Cas No. | 181769-57-3 |
Formula | C26H34N4O5 |
Synonyms | Z-L-Nva-CONH-CH2-2-Py |
Solubility | ≤16mg/ml in ethanol;16mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | [3-methyl-1-[[[1-[oxo[(2-pyridinylmethyl)amino]acetyl]butyl]amino]carbonyl]butyl]-carbamic acid, phenylmethyl ester |
SDF | Download SDF |
Canonical SMILES | O=C(NC(CC(C)C)C(NC(CCC)C(C(NCC1=NC=CC=C1)=O)=O)=O)OCC2=CC=CC=C2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
Cell experiment:[1] | |
Cell lines |
Aplysia neurons |
Reaction Conditions |
200 μM calpain inhibitor XII |
Applications |
Calpain inhibitor XII inhibited voltage-gated potassium conductance and moderately reduced the sodium conductance, which consequently led to spike broadening and increased calcium influx. Such alterations of the excitable membrane properties may alter the normal patterns of neuronal and muscle electrical activities. |
Note |
The technical data provided above is for reference only. |
References: 1. Khoutorsky A, Spira ME. Calpain inhibitors alter the excitable membrane properties of cultured aplysia neurons. Journal of Neurophysiology, 2008, 100(5): 2784-2793. |