Identification | Back Directory | [Name]
CALPAIN INHIBITOR I | [CAS]
110044-82-1 | [Synonyms]
LLNL ALLN MG 101 ac-llnl-cho MG-101 (ALLN) InSolution? ALLN AC-LL-NORLEUCINAL Ac-Leu-Leu-Nle-al CALPAIN INHIBITOR AC-LEU-LEU-NLE-CHO CALPAIN INHIBITOR I AC-LEU-LEU-NORLEUCINAL AC-LEU-LEU-NLE-ALDEHYDE Calpain Inhibitor I,96% N-AC-LEU-LEU-NORLEUCINAL N-ACETYL-LEU-LEU-NLE-CHO AC-LEU-LEU-L-NORLEUCINAL Calpain Inhibitor I, ALLN N-Acetyl-Leu-Leu-Norleu-al ACETYL-LEU-LEU-NORLEUCINAL AC-LEU-LEU-NLE-H (ALDEHYDE) N-ACETYL-LEU-LEU-NORLEUCINAL acetylleucyl-leucyl-norleucinal ACETYL-L-LEUCYL-L-LEUCYL-L-NORLEUCINAL N-ACETYL-L-LEUCYL-L-LEUCYL-L-NORLEUCINAL N-Acetyl-L-leucine-L-leucine-L-norleucinal N-Acetyl-L-leucinyl-L-leucinyl-L-norleucinal N-acetyl-L-leucyl-N-[(1S)-1-formylpentyl]-L-Leucinamide Calpain Inhibitor Ⅰ 〔N-Acetyl-L-leucyl-L-leucyl-L-norleucinal〕 ALLN, Ac-LLnL-CHO, MG-101, N-Acetyl-Leu-Leu-Norleu-al, N-Acetyl-L-leucyl-L-leucyl-L-norleucinal Ac-LLnL-CHO, ALLN, MG-101, N-Acetyl-Leu-Leu-Norleu-al, N-Acetyl-L-leucyl-L-leucyl-L-norleucinal | [EINECS(EC#)]
999-999-2 | [Molecular Formula]
C20H37N3O4 | [MDL Number]
MFCD00065505 | [MOL File]
110044-82-1.mol | [Molecular Weight]
383.53 |
Chemical Properties | Back Directory | [Appearance]
white to off-white powder | [Melting point ]
182 °C | [Boiling point ]
510.42°C (rough estimate) | [density ]
1.1322 (rough estimate) | [refractive index ]
1.6300 (estimate) | [storage temp. ]
−20°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. |
Hazard Information | Back Directory | [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. | [Definition]
ChEBI: A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence. | [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. | [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. | [General Description]
Calpain Inhibitor I is a strong, competitive inhibitor of the Ca2+-dependent neutral cysteine proteases calpain I and calpain II. | [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 |
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