DATASHEET
Formulation
Solid
Storage:
Stable for 2 years after receipt when stored at -20°C.
Product Information:
CAS Number: 847499-27-8
Molecular formula: C21H28BN3O5
Molecular weight: 413.3
Purity: >95% (1H-NMR)
Appearance: White solid.
Solubility: Soluble in DMSO (20mg/ml) or ethanol (20mg/ml). Slightly soluble in chloroform or methanol. Poorly soluble in water (<1mg/ml).
InChiKey: SJFBTAPEPRWNKH-CCKFTAQKSA-N
SMILES: CC(C)C[C@@H](B(O)O)NC([C@H]([C@H](O)C)NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)=O
Description:
Potent, selective, reversible orally bioavailable proteasome inhibitor. Synthetic P2 threonine boronic acid. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=3.8nM). Cross-reacts and inhibits the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=~70nM). Displays similar potency for the chymotrypsin-like activity of the proteasome compared to bortezomib. Exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors and bone marrow-derived stromal cells relative to bortezomib (Prod. No. bs-75509C). Anticancer compound effective against multiple myeloma in vivo. In vitro, blocks the growth of representative human solid and hematological tumor cell lines (IC50s=5.6-34nM). Shown to down-modulate NF-kappaB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.