Physical Appearance:  White solid

Molecular Formula:  C₁₅H₂₄N₂O₇S

Molecular Weight:  376.4

Purity:  99% (NMR)

Solubility:  Soluble in water (10mg/ml)

Storage:  Store, as supplied, at -20°C for up to 1 year.  Store solutions at -20°C for up to 3 months.

Description:  A potent and selective proteasome inhibitor which affects all three ATP-independent activities of 2OS proteasome (inhibitions of chymotrypsin- and trypsin-like are irreversible; pep.glu-like is reversible). Highly specific, viz. 100µM has no effect on chymotrypsin, trypsin or papain after 48 hrs. Radiolabeling of cells/crude extracts labels primarily X/MB1 proteasome subunit (24 kD) and to a lesser extent, the proteasome α-chain (~30kD). Inhibits NF-κB activation (IC₅₀ = 10µM). Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells. The product is not sterile.

References:

1.      G. Fenteany et al. Science 1995 268 726

2.      J. Adams and R. Stein Am.Rep.Med.Chem. 1996 31 279

3.      G. Fenteany et al. Proc. Natl. Acad. Sci.USA 1994 91 3358

The pharmacological and toxicological properties of this product have not been fully investigated.  Exercise caution in use and handling. This product must not be used in humans.