Calpain Inhibitor I Chemical Properties

Melting point:

182 °C

Boiling point:

510.42°C (rough estimate)

Density 

1.1322 (rough estimate)

refractive index 

1.6300 (estimate)

storage temp. 

2-8°C

solubility 

DMSO: soluble

form 

powder

pka

13.53±0.46(Predicted)

color 

white

biological source

synthetic (organic)

Water Solubility 

Soluble in dimethyl sulfoxide, ethanol, methanol. Insoluble in water, and aqueous buffers.

BRN 

7656053

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

F 

3-10

HS Code 

29241900

MSDS

• Language:English Provider:SigmaAldrich
• Language:English Provider:ACROS

Calpain Inhibitor I Usage And Synthesis

Description

ALLN (110044-82-1) is a cell-permeable, peptide aldehyde inhibitor of calpain I (Ki=190 nM), calpain II (Ki=150 nM), cathepsin L (Ki=0.5 nM) and other neutral cysteine proteases.1?Inhibits cell cycle progression at G1/S?and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation.2?Inhibits proteolytic degradation of IκBα and IκBβ in RAW macrophages induced with LPS.3?Blocks AIF-mediated necroptosis.4?Cell permeable.

Chemical Properties

white to off-white powder

Uses

Calpain inhibitor I reversibly blocks the calcium-dependent neutral cysteine protease calpain I. Calpains have been implicated in various cellular processes, including cell proliferation, apoptosis, and cell differentiation.

Uses

Calpain inhibitor I inhibits calpain, which activates myosin light chain kinase and protein kinase C by partial proteolysis. The inhibitor should be membrane permeable due to low molecular weight and lack of charged residues.
Calpain Inhibitor I is used for western blotting methods.

Uses

It inhibits apoptosis in thymocytes and metamyelocytes. It also inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. ALLN inhibits the proteolysis of IκBα and IκBβ by the ubiquitin-proteasome complex. ALLN also prevents nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene.

Definition

ChEBI: A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence.

General Description

Calpain Inhibitor I is a strong, competitive inhibitor of the Ca²⁺-dependent neutral cysteine proteases calpain I and calpain II.

Biological Activity

Calpain inhibitor (IC 50 = 0.09 μ M) that activates p53-dependent apoptosis in tumor cell lines. Increases activated p53, p21 and caspase levels and promotes cell cycle arrest through inhibition of cyclin D degradation in vitro . Also attenuates ischemia/reperfusion injury in cardiomyocytes, hepatocytes and renal tubular cells through downregulation of iNOS and COX-2 expression.

Biochem/physiol Actions

Calpain Inhibitor I inhibits tumor necrosis factor-induced (TNF-induced) cleavage of Poly (ADP-ribose) polymerase (PARP) and calpastatin in apoptosis. It also inhibits oxygen/glucose deprivation (OGD) induced cleavage of caspase-12 and Bcl-xL..

References

[1] T SASAKI. Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins.[J]. Journal of enzyme inhibition, 1990, 3 3: 195-201. DOI:10.3109/14756369009035837
[2] S W SHERWOOD. In vivo inhibition of cyclin B degradation and induction of cell-cycle arrest in mammalian cells by the neutral cysteine protease inhibitor N-acetylleucylleucylnorleucinal.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1993, 90 8: 3353-3357. DOI:10.1073/pnas.90.8.3353
[3] N-acetyl-leucinyl-leucinyl-norleucinal inhibits lipopolysaccharide-induced NF-kappaB activation and prevents TNF and IL-6 synthesis in vivo
[4] LEI SHANG. Calpain: a molecule to induce AIF-mediated necroptosis in RGC-5 following elevated hydrostatic pressure.[J]. BMC Neuroscience, 2014, 15: 63. DOI:10.1186/1471-2202-15-63

Calpain Inhibitor I(110044-82-1)Related Product Information

• Calpain Inhibitor I
• CALPAIN INHIBITOR I,CALPAIN INHIBITOR
• CALPAIN INHIBITOR IV
• CALPAIN INHIBITOR III
• MET-ALA-GLY-ARG-SER-GLY-ASP-SER-ASP-GLU-ASP-LEU-LEU-LYS-ALA-VAL
• (TYR0)-KALIURETIC PEPTIDE (HUMAN)
• H-PRO-ALA-VAL-ASP-LEU-LEU-LYS-ASN-TYR-MET-GLN-LEU-GLY-LYS-GLN-OH
• ASP-GLU-ASP-LEU-LEU-LYS-ALA-VAL-ARG-LEU-ILE-LYS-PHE-LEU-TYR-GLN-SER-ASN
• PEPTITERGENT PD1
• H-PRO-PRO-GLU-ASP-PRO-ALA-VAL-ASP-LEU-LEU-LYS-ASN-TYR-MET-GLN-LEU-GLY-LYS-GLN-GLN-OH
• H-MET-PRO-THR-ALA-PRO-PRO-GLU-ASP-PRO-ALA-VAL-ASP-LEU-LEU-LYS-OH
• KALIURETIC PEPTIDE (HUMAN)
• SPFK
• H-SER-LEU-LEU-LYS-OH
• H-PRO-PRO-GLU-ASP-PRO-ALA-VAL-ASP-LEU-LEU-LYS-ASN-TYR-MET-GLN-OH
• PREPRO-ANF (104-116), HUMAN
• PSTAIR peptide
• GLU-ASP-LEU-LEU-LYS-ALA-VAL-ARG-LEU-ILE-LYS