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Enzymes for Research, Diagnostic and Industrial Use

Bortezomib (Velcade)

Cat No.
CEI-0216
Description
Bortezomib (Velcade) can inhibit proteasome with Ki of 0.6 nM.
Alias
MG-341, PS-341
CAS No.
179324-69-7
Molecular Weight
384.24
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
MG-341, PS-341
Targets
proteasome
Molecular Formula
C19H25BN4O4
Solubility
DMSO 77 mg/mL Water
In vitro
As a small, cell-permeable dipeptidylboronic acid derivative, bortezomib (Velcade, MG-341, PS-341) can reversibly inhibits the chymotrypsin-like activity of the proteasome by binding tightly to the active sites of the enzyme with Ki of 0.6 nM. PS-341 Induces Apoptosis and IkappaBalpha Degradation and Inhibits p44/42 MAPK Activation in MM Cells. In the NCI-60 cell lines, bortezomib showed growth inhibitory and cytotoxic activity for many human tumor cell types, with an average GI 50 of 3.8 nM across the 60 cell lines. Bortezomib (Velcade, MG-341, PS-341) showed inhibition in multiple myeloma. PS-341 can inhibit U266, IM-9, and Hs Sultan cells with IC50 of 3 mM, 6 mM and 20 nM.
In vivo
TC-1(P3) tumor-bearing mice treated with bortezomib prior to vaccination with E7-DC-1STAT3-/- demonstrated enhanced generation of E7-specific CD8+ T cells and prolonged survival. Bortezomib can potently induce apoptosis and suppressed the growth of NPC xenografts in nude mice.
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