Potent, irreversible inhibitor of all the 3 proteolytic activities of the mammalian 20S proteasome. -beta5 subunit: chymotrypsin-like (EC50 = 3.5nM) -beta2 subunit: trypsin-like (EC50 = 28nM) -beta1 subunit: caspase-like or peptidyl-glutamyl peptide-hydrolyzing (PGPH) (EC50 = 430nM) Potent anticancer compound. Triggers apoptosis, with distinct proteasome activity and mechanism of action compared to bortezomib (Velcade). Most potent suppressor of NF-kB activation, compared with bortezomib, MG-132, N-acetyl-leucyl-leucyl-norleucinal (ALLN) and lactacystin. Inhibitor of TNF-alpha, IL-1, IL-6, ICAM-1 and VEGF synthesis. Displays a longer inhibition duration than bortezomib. Potent antileukemic activity against bortezomib-resistant leukemia cells. Solubility: Soluble in DMSO. Do not dissolve in methanol or ethanol. Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molekulargewicht:
313.8
Reinheit:
95% (HPLC)
Formulierung:
Supplied as a white solid.
CAS Nummer:
[437742-34-2]
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
