Calpain Inhibitor I
Calpain Inhibitor I Basic information
- Product Name:
- Calpain Inhibitor I
- Synonyms:
-
- acetylleucyl-leucyl-norleucinal
- N-AC-LEU-LEU-NORLEUCINAL
- N-ACETYL-LEU-LEU-NLE-CHO
- N-ACETYL-L-LEUCYL-L-LEUCYL-L-NORLEUCINAL
- N-ACETYL-LEU-LEU-NORLEUCINAL
- MG 101
- CALPAIN INHIBITOR I;AC-LLNL-CHO;ALLN
- LLNL
- CAS:
- 110044-82-1
- MF:
- C20H37N3O4
- MW:
- 383.53
- EINECS:
- 999-999-2
- Product Categories:
-
- inhibitor
- peptides
- C-CH
- Cell Biology
- Cell Signaling and Neuroscience
- ProteasomeInhibitors
- Cell Signaling Enzymes
- Chemical Synthesis
- Endoplasmic Reticulum Stress
- Enzyme Inhibitors
- Enzyme Inhibitors by Enzyme
- Enzymes
- Inhibitors
- Intracellular Protein Degradation
- Calpain I
- Calpain I Inhibitors
- Cathepsin L
- Lysosomal Proteases
- Nitric Ox
- A to C
- Aldehydes
- and Substrates
- Apoptosis Enzymes
- Application Index
- Bioactive Small Molecules
- Biochemicals and Reagents
- Building Blocks
- C13-C60
- Calpain
- Substrates
- Calpain and Proteasome Inhibitors
- Calpain II
- Calpain II Inhibitors
- Carbonyl Compounds
- Cathepsin B
- Cathepsin/Granzyme Inhibitors &
- Mol File:
- 110044-82-1.mol
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
- 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.
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
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.
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.
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
Calpain Inhibitor ISupplier
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- 010-82848833 400-666-7788
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- shchemsky@sina.com
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