Description
An inhibitor of chymotrypsin-like proteasome activity (IC50 = 3.8 nM); pre-treatment in vitro with a concentration of 20 nM inhibits IκBα degradation, NF-κB activation, and the expression of NF-κB-regulated genes, including IκBα, XIAP, TNF-α, IL-1β, ICAM1, and VEGF; induces apoptosis in multiple myeloma cell lines and inhibits proliferation in a panel of human hematologic and solid tumor cell lines (IC50s = 5.6-34.2 nM); reduces tumor weight in an RPMI 8226 human multiple myeloma mouse xenograft model when administered intravenously at doses ranging from 1.5-4 mg/kg twice daily and leads to complete tumor regression at a chronic oral dose of 13 mg/kg; efficacious in a mouse model of fata lupus nephritis
Formal name: B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2-pyridinyl)carbonyl]amino]butyl]amino]-3-methylbutyl]-boronic acid
Synonyms: CEP-18770
Molecular weight: 413.3
CAS: 847499-27-8
Purity: ≥95%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|NF-κB Signaling||Research Area|Cancer|Transcription Factors|NF-κB||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Autoimmunity|Lupus
