Clasto-Lactacystin ?-lactone

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Clasto-Lactacystin ?-lactone Basic information
Product Name:Clasto-Lactacystin ?-lactone
Synonyms:OMURALIDE;LACTACYSTIN, CLASTO-, BETA-LACTONE;BETA-CLASTOLACTACYSTIN;CLASTO-LACTACYSTIN BETA-LACTONE;1R-[1S-1HYDROXY-2-METHYLPROPYL]-4R-METHYL-6-OXA-2-AZABICYCLO[3.2.0]HEPTANE-3,7-DIONE;Clasto-lactacystin (OMuralide);(1R,4R,5S)-1-[(1S)-1-Hydroxy-2-Methylpropyl]-4-Methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione;6-Oxa-2-azabicyclo[3.2.0]heptane-3,7-dione, 1-[(1S)-1-hydroxy-2-methylpropyl]-4-methyl-, (1R,4R,5S)-
CAS:154226-60-5
MF:C10H15NO4
MW:213.23
EINECS:
Product Categories:Calpain and Proteasome InhibitorsProteasome, Calpain and Lysosomal Proteases;InhibitorsProtease Inhibitors;Proteasome inhibitor;Proteasome inhibitorEnzyme Inhibitors by Enzyme;Intracellular Protein Degradation;Nitric Oxide and Cell Stress;P to;Protease Inhibitor Specificity Index;Proteasomes;ProteasomeInhibitors;Inhibitors
Mol File:154226-60-5.mol
Clasto-Lactacystin ?-lactone Structure
Clasto-Lactacystin ?-lactone Chemical Properties
Melting point 186-187°C
Boiling point 440.815±40.00 °C(Press: 760.00 Torr)(predicted)
density 1.280±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
storage temp. -20°C
solubility DMF, Ethanol, Hot Ethyl Acetate, Methanol, Pyridine
form White solid
pka13.332±0.20(predicted)
color White
InChI1S/C10H15NO4/c1-4(2)6(12)10-7(15-9(10)14)5(3)8(13)11-10/h4-7,12H,1-3H3,(H,11,13)/t5-,6+,7+,10-/m1/s1
InChIKeyFWPWHHUJACGNMZ-NBBQQVJHSA-N
SMILES[H][C@@]12OC(=O)[C@@]1(NC(=O)[C@@H]2C)[C@@H](O)C(C)C
Safety Information
Hazard Codes T
Risk Statements 20/21/22-37/38-41-36/37/38-25
Safety Statements 16-26-36/37/39-45
RIDADR UN 2811 6.1 / PGIII
WGK Germany 2
Storage Class11 - Combustible Solids
Hazard ClassificationsEye Irrit. 2
MSDS Information
ProviderLanguage
SigmaAldrich English
Clasto-Lactacystin ?-lactone Usage And Synthesis
Chemical PropertiesWhite Solid
UsesA cell permeable, irreversible proteasome inhibitor. It is 20-fold more potent than Lactacystin. Lactacytstin spontaneously converts to clasto-lactacystin in biological systems. Clasto-lactacystin is the only cell permeable form of lactacystin. Induces neurite growth and inhibits cell cycle progression similar to lactacytin.
UsesClasto-Lactacystin β-lactone has been used as a proteasomal inhibitor.
Usesclasto-Lactacystin beta-lactone is a 20S proteasome and cathepsin A inhibitor.
Biological Activitycell-permeable. a highly specific, potent and irreversible proteasome inhibitor. lactacystin (cat. no. 1709-200) acts as a precursor for clasto-lactacystin β-lactone and the latter compound is at least 10 times more active than the parent lactacystin
Biochem/physiol ActionsClasto-Lactacystin β-lactone (cLβL) is synthesized from lactacystin. It is cell-permeable and cLβL acts on the N-terminal threonine of subunit proteasome β -subunit X It also inhibits 20S proteasome activity in Haloferax volcaniiby acting in the N-threonine residue of the β -type subunits.
Clasto-Lactacystin ?-lactone Preparation Products And Raw materials
Raw materials(3R,4S,5R)-4-HYDROXY-5-[(1S)-1-HYDROXY-2-METHYLPROPYL]-3-METHYL-2-PYRROLIDINONE-5-CARBOXYLIC ACID
Tag:Clasto-Lactacystin ?-lactone(154226-60-5) Related Product Information
Ethyl D-(-)-pyroglutamate 2-Methyl-D-serine (2R,3S)-(-)-2-Amino-3-hydroxy-4-methylpentanoic acid (S)-4-Hydroxy-2-pyrrolidinone CIS-3-HYDROXY-DL-PROLINE 2-Oxetanone D-Pyroglutamic acid BETA-BUTYROLACTONE 5-Hydroxymethylpyrrolidin-2-one DL-2-ISOBUTYLSERINE LACTACYSTIN DIPROPYLGLYCINE dl-3-hydroxynorvaline (2R,4R)-4-METHYL-2-PYROOLIDINE CARBOXYLIC ACID H-ALPHA-ME-D-LEU-OH 3-OXETANAMINE, 3-METHYL- H-ALPHA-ME-D-PRO-OH 5,5-Dimethyl-2-pyrrolidinone