110044-82-1 Usage
Uses
Used in Cellular Biology Research:
Calpain Inhibitor I is used as a research tool for studying the role of calpains in cellular processes, such as cell proliferation, apoptosis, and cell differentiation. Its ability to reversibly block calpain I and II activity allows researchers to investigate the specific functions and mechanisms of these proteases in various cell types.
Used in Apoptosis Inhibition:
Calpain Inhibitor I is used as an apoptosis inhibitor in thymocytes and metamyelocytes. By inhibiting calpain activity, it helps prevent cell death and can be useful in studying the mechanisms of apoptosis and identifying potential therapeutic targets for conditions involving excessive cell death.
Used in Cell Cycle Regulation:
Calpain Inhibitor I is used as a cell cycle regulator in CHO cells, where it inhibits cell cycle progression at the G1/S border and metaphase/anaphase by inhibiting cyclin B degradation. This application aids in understanding the role of calpains in cell cycle regulation and their potential involvement in diseases related to uncontrolled cell proliferation.
Used in Inflammation and Immune Response:
Calpain Inhibitor I is used as an inhibitor of the proteolysis of IκBα and IκBβ by the ubiquitin-proteasome complex in RAW macrophages induced with LPS. This application helps in studying the role of calpains in inflammation and immune response, as well as their potential as therapeutic targets for inflammatory diseases.
Used in Western Blotting Methods:
Calpain Inhibitor I is used in western blotting methods to inhibit calpain activity during sample preparation, ensuring accurate protein detection and analysis. Its membrane permeability and low molecular weight make it suitable for this application.
Used in Drug Development:
Calpain Inhibitor I can be used in the development of drugs targeting calpain-mediated processes, such as neurodegenerative diseases, muscular dystrophies, and cancer. Its ability to inhibit calpain activity makes it a potential candidate for therapeutic intervention in these conditions.
Used in Nitric Oxide Production Inhibition:
Calpain Inhibitor I is used to prevent nitric oxide production by activated macrophages by interfering with the transcription of the inducible nitric oxide synthase gene. This application can be useful in studying the role of calpains in the regulation of nitric oxide production and its implications in various physiological and pathological processes.
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
Check Digit Verification of cas no
The CAS Registry Mumber 110044-82-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,0,0,4 and 4 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 110044-82:
(8*1)+(7*1)+(6*0)+(5*0)+(4*4)+(3*4)+(2*8)+(1*2)=61
61 % 10 = 1
So 110044-82-1 is a valid CAS Registry Number.
InChI:InChI=1/C20H37N3O4/c1-7-8-9-16(12-24)22-19(26)18(11-14(4)5)23-20(27)17(10-13(2)3)21-15(6)25/h12-14,16-18H,7-11H2,1-6H3,(H,21,25)(H,22,26)(H,23,27)/t16-,17-,18-/m0/s1
110044-82-1Relevant articles and documents
Bivalent inhibitors of the proteasome
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, (2008/06/13)
A bivalent proteasome inhibitor of the general formula IX-CH(R1)-NH-[P]n-Y-Z-Y'-[P']m-NH-CH(R1')-X' wherein X and X' are identical or different and are groups selected from aldehyde, boronic acid, boronic acid ester, ketoaldehyde, ketoester, ketoamide, chloromethylketone, trifluoromethylketone, diazomethane;R1 and R1' are identical or different and correspond to the specificity of the S1 enzyme subsite for chymotrypsin- or trypsin-like or PGPH activity of the proteasome, selected from hydrophobic side chains of L- or D-natural and -unnatural amino acids, or amino-, guanido-, amidino-alkyl- or cycloalkyl-, alkaryl-, aralkyl residues and carboxy-alkyl- or aryl- or alkaryl- or aralkyl residues;P and P' are identical or different and correspond to the P2 to P7 substrate positions and are natural or unnatural L- or D-amino acids with hydrophobic or hydrophylic or charged side chains;m and n are identical or different and are 0, 1, 2, 3, 4, 5 or 6;Y and Y' are identical or different and correspond to the formula CO-(A)-(B) where (A) is an alkyl, alkenyl, cycloalkyl, alkaryl, aralkyl or heteroaromatic group and (B) is CO or NH or omitted;and Z is O-CH2-CH2-(O-CH2-CH2)n-O, OC-CH2-(O-CH2-CH2)n-1-O-CH2-CO or NH-CH2-CH2-(O-CH2-CH2)n-NH with n varying from 4 to 50 has interesting properties for various drug applications.
Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
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, (2008/06/13)
Use of a compound represented by the following general formula (I): wherein R1 represents a straight or branched acyl group having 2 to 10 carbon atoms, a branched cyclic or bridged cyclic alkyloxycarbonyl group having 4 to 15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)-ethyloxycarbonyl group, a p-toluenesulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutanoyl group; R2 represents a hydrogen atom or forms a phthaloyl group together with R1; R3 represents an isobutyl group, an n-butyl group or an isopropyl group; R? represents an n-butyl group or an isobutyl group; X represents a direct bond, a methionine residue, a leucine residue or a norleucine residue; and H at the C-terminal means that the carboxyl group is reduced in the form of the aldehyde; as an active ingredient for the preparation of a pharmaceutical composition useful in preventing or treating malignant hypercalcemia, bone Paget's disease or osteoporosis.
