Calpain Inhibitor I

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

The Uses of Calpain Inhibitor I

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.

The Uses of Calpain Inhibitor I

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.

The Uses of Calpain Inhibitor I

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.

What are the applications of Application

ALLN is a peptide aldehyde inhibitor of calpains and cathepsins

What are the applications of Application

Calpain Inhibitor I is a calpain and cathepsin inhibitor

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) Sasaki?et al.?(1990),?Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins; J. Enzyme Inhib.?3?195 2) Sherwood?et al. (1993)?In vivo inhibition of cyclin B degradation and induction of cell-cycle arrest in mammalian cells by the neutral cysteine protease inhibitor N-acetylleucylleucylnorleucinal; Proc. Natl. Acad. Sci USA?90?3353 3) Schow and Joly (1997),?N-acetyl-leucinyl-leucinyl-norleucinal inhibits lipopolysaccharide-induced NF-kappaB activation and prevents TNF and IL-6 synthesis in vivo; Cell Immunol.?175?199 4) Shang?et al.?(2014)?Calpain: a molecule to induce AIF-mediated necroptosis in RGC-5 following elevated hydrostatic pressure; BMC Neurosci.?15?63