Formulation: A solid
Formal Name: B-[(1R)-2-(3-benzofuranyl)-1-[[(1S,2R,4R)-7-oxabicyclo[2.2.1]hept-2-ylcarbonyl]amino]ethyl]-boronic acid
Purity: ≥98%
Formula Markup: C17H20BNO5
Formula Weight: 329,2
Shelf life (days): 1460
CAS Number: 2285330-15-4
Notes: M-3258 is an inhibitor of the immunoproteasome subunit large multifunctional peptidase 7 (LMP7; IC50 = 4.1 nM).{68455} It is selective for LMP7 over the 20S proteasomal catalytic subunits β1, -β2, and -β5 (IC50s = >10,000, 2,519, and >10,000 nM, respectively), as well as LMP2 and proteosome subunit beta type 10 (PSMB10; IC50s = >10,000 nM for both). It increases ubiquitinated protein levels (EC50 = 1,980 nM) and induces apoptosis in MM.1S multiple myeloma cells (EC50 = 420 nM). M-3258 (10 mg/kg per day) reduces tumor volume in U266B1, OPM-2, and RPMI-8226 mouse xenograft models of multiple myeloma.