A cell-permeable tetrapeptidylsulfonylfluoride-based irreversible proteasome inhibitor that selectively inhibits the hydrolysis of Suc-LLVY-AMC by the beta5 chymotrypsin-like activity (IC50 = 7nM using yeast 20S proteasome), while exhibiting much reduced potency against Z-LLE-AMC hydrolysis by the beta1 caspase-like activity or Z-LLR-AMC hydrolysis by the beta2 trypsin-like activity (29% and 75% inhibition, respectively, with 200uM inhibitor). One hour inhibitor treatment at 5uM in HEK cultures is shown to completely abolish beta5 labeling by the proteasome probe MV151, while only partial MV151 blockage is seen with beta1 and beta2 at an inhibitor concentration of 50uM. Synonyms: Cbz-Leu-Leu-Leu-Leu-psi-[CH2SO2]-F, Cbz-Leu4-SF, Cbz-LLLL-SF, Z-Leu4-SF, Z-L4-SF Molecular Formula: C32H53FN4O7S Solubility: DMSO Primary Target: beta-5 chymotrypsin-like activity of 20S proteasome Storage and Stability: Store at -20C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Reinheit:
98% (HPLC)
Formulierung:
Supplied as a white powder.
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