Targeted elimination of damaged or unwanted proteins via the ubiquitin-proteasome pathway is fundamental to the control of many essential cell functions, including cell-cycle progression, gene transcription, and apoptosis. [1] The dipeptide boronic acid inhibitor bortezomib effectively inhibits proteasome activity (Ki-0.6 nM) but has little affinity for other proteases (e.g., for chymotrypsin, Ki=320 nM, and for thrombin, Ki=13,000 nM). [2] The level of apoptosis was 80% to 90% in cells treated with bortezomib plus SN-38, vs. 10% with either agent alone. [3]
Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.
The cellular ataxia telangiectasia-mutated kinase promotes epstein-barr virus lytic reactivation in response to multiple different types of lytic reactivation-inducing stimuli.
Drug resistance to inhibitors of the human double minute-2 E3 ligase is mediated by point mutations of p53, but can be overcome with the p53 targeting agent RITA.
The clinically approved proteasome inhibitor PS-341 efficiently blocks influenza A virus and vesicular stomatitis virus propagation by establishing an antiviral state.
Proteasome-dependent activation of mammalian target of rapamycin complex 1 (mTORC1) is essential for autophagy suppression and muscle remodeling following denervation.
The Raf/MEK/extracellular signal-regulated kinase 1/2 pathway can mediate growth inhibitory and differentiation signaling via androgen receptor downregulation in prostate cancer cells.
Secretory phospholipase A2-IIa is a target gene of the HER/HER2-elicited pathway and a potential plasma biomarker for poor prognosis of prostate cancer.
NFκB pathway is down-regulated by 1α,25(OH)(2)-vitamin D(3) in endothelial cells transformed by Kaposi sarcoma-associated herpes virus G protein coupled receptor.
Agents That Stabilize Mutated von Hippel–Lindau (VHL) Protein Results of a High-Throughput Screen to Identify Compounds That Modulate VHL Proteostasis.
Data from [Carcinogenesis 2010;31, 1948–1955]
Bortezomib (Velcade) purchased from Selleck
I am very satisfied with your product and costumer service. Bortezomib works very well in our assay, it is comparably cheaper than other inhibitors that we tested is more reliable for our assays. We see a great effect by using 10nM concentration.
Dr. Alexandra SegrefCECAD Cologne, Germay
We are very much satisfied by the service of Selleckchem. The products were of good quality and very useful for our research in collaboration with the Cancer Research Institute of Oslo.
Manuel Alvaro Neto Coelho, PhDProfessor of Chemical Engineering, University of Porto
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