An LMP7 inhibitor
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M-3258

Item No. 38160

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
B-[(1R)-2-(3-benzofuranyl)-1-[[(1S,2R,4R)-7-oxabicyclo[2.2.1]hept-2-ylcarbonyl]amino]ethyl]-boronic acid
CAS Number
2285330-15-4
Molecular Formula
C17H20BNO5
Formula Weight
329.2
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
λmax
248 nm
SMILES
OB(O)[C@@H](NC([C@H]1[C@@](CC2)([H])O[C@@]2([H])C1)=O)CC3=COC4=CC=CC=C34
InChi Code
InChI=1S/C17H20BNO5/c20-17(13-8-11-5-6-15(13)24-11)19-16(18(21)22)7-10-9-23-14-4-2-1-3-12(10)14/h1-4,9,11,13,15-16,21-22H,5-8H2,(H,19,20)/t11-,13-,15+,16+/m1/s1
InChi Key
RFQDLTYXNINJON-OYNZBZHQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    M-3258 is an inhibitor of the immunoproteasome subunit large multifunctional peptidase 7 (LMP7; IC50 = 4.1 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sanderson, M.P., Friese-Hamim, M., Walter-Bausch, G., et al. M3258 is a selective inhibitor of the immunoproteasome subunit LMP7 (β5i) delivering efficacy in multiple myeloma models. Mol. Cancer Ther. 20(8), 1378-1387 (2021).