539185

Proteasome Inhibitor XX, GL5 - CAS 146304-91-8 - Calbiochem

The Proteasome Inhibitor XX, GL5, also referenced under CAS 146304-91-8, controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Proteasome Inhibitor XX, GL5 - CAS 146304-91-8 - Calbiochem, 5-(5-Methyl-2-(methylthio)thiophen-3-yl)-1,3,4-oxathiazol-2-one
• Empirical Formula (Hill Notation): C₈H₇NO₂S₃
• CAS Number: 146304-91-8
• Molecular Weight: 245.34
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: brown
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A cell-permeable thienyl-oxathiazolone compound that effectively kills non-replicating Mycobacterium tuberculosis (~320- or 12,600-fold drop in BCG titre over 4 days by 50 µM GL5 with or without 50 µM DETA-NO, respectively) by selectively inhibiting its proteasome activity (by ~90% over 4 hours with 50 µM GL5) in a substrate-competitive and irreversible manner, while exhibiting little activity against trypsin, cathepsin B, MMP-2, or human 20S proteasome β1/2/5. GL5 displays no antibacterial activity against M. avium-intracellulare, Staphylococcus aureus, Salmonella enterica var. Typhimurium, or Pseudomonas aeruginosa. Although GL5 is known to reversibly inhibit α-chymotrypsin (K_i = 0.064 µM), it exerts no apparent toxicity to human or monkey cells. GL5 is reasonably stable in RPMI medium (t_1/2 = 110 mins at 37°C) albeit its moderate chemical reactivity toward glutathione (12.7% over 30 min at pH 7.0, RT; 10 µM GL5 and 25 µM GSH).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Lin. G., et al. 2009. Nature461, 621.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 10-13 - German Storage Class 10 to 13