474780

MG-115

Potent reversible proteasome inhibitor (K_i = 21 nM and 35 nM for 20S and 26S proteasome, respectively).

• Synonym(s): MG-115, Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII
• Empirical Formula (Hill Notation): C₂₅H₃₉N₃O₅
• CAS Number: 133407-86-0
• Molecular Weight: 461.59
• MDL number: MFCD00274411
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥90% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥90% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: N([C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC)C=O)C(=O)OCc1ccccc1
• InChI: 1S/C25H39N3O5/c1-6-10-20(15-29)26-23(30)21(13-17(2)3)27-24(31)22(14-18(4)5)28-25(32)33-16-19-11-8-7-9-12-19/h7-9,11-12,15,17-18,20-22H,6,10,13-14,16H2,1-5H3,(H,26,30)(H,27,31)(H,28,32)/t20-,21-,22-/m0/s1
• InChI key: QEJRGURBLQWEOU-FKBYEOEOSA-N

Description

General description

Potent reversible proteasome inhibitor (K_i = 21 nM and 35 nM for 20S and 26S proteasome, respectively). Specifically inhibits the chymotrypsin-like activity of the proteasome and induces apoptosis in Rat-1 and PC12 cells.

Biochem/physiol Actions

Cell permeable: no

Primary Target
20S proteasome

Product does not compete with ATP.

Reversible: yes

Target K_i: 21 nM and 35 nM for 20S and 26S proteasome, respectively

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Lopes, U.G., et al. 1997. J. Biol. Chem. 272, 12893.
Lee, D.H., and Goldberg, A.L. 1996. J. Biol. Chem.271, 27280.
Palombella, V.J., et al. 1994. Cell 78, 773. Rock, K.L., et al. 1994. Cell 78, 761.
Vinitsky, A., et al. 1992. Biochemistry 31, 9421.

Z-Leu-Leu-Nva-CHO

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable