Synonym
M3258; M 3258; M-3258;
IUPAC/Chemical Name
((S)-2-(benzofuran-3-yl)-1-((1R,2R,4S)-7-oxabicyclo[2.2.1]heptane-2-carboxamido)ethyl)boronic acid
InChi Key
RFQDLTYXNINJON-KSZJFAHPSA-N
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+/m0/s1
SMILES Code
O=C([C@H]1[C@@](O2)([H])CC[C@@]2([H])C1)N[C@@H](B(O)O)CC3=COC4=CC=CC=C34
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
329.16
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Sloot W, Glaser N, Hansen A, Hellmann J, Jaeckel S, Johannes S, Knippel A, Lai V, Onidi M. Improved nonclinical safety profile of a novel, highly selective inhibitor of the immunoproteasome subunit LMP7 (M3258). Toxicol Appl Pharmacol. 2021 Oct 15;429:115695. doi: 10.1016/j.taap.2021.115695. Epub 2021 Aug 20. PMID: 34419493.
2: Klein M, Busch M, Friese-Hamim M, Crosignani S, Fuchss T, Musil D, Rohdich F, Sanderson MP, Seenisamy J, Walter-Bausch G, Zanelli U, Hewitt P, Esdar C, Schadt O. Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i). J Med Chem. 2021 Jul 22;64(14):10230-10245. doi: 10.1021/acs.jmedchem.1c00604. Epub 2021 Jul 6. PMID: 34228444.
3: Sanderson MP, Friese-Hamim M, Walter-Bausch G, Busch M, Gaus S, Musil D, Rohdich F, Zanelli U, Downey-Kopyscinski SL, Mitsiades CS, Schadt O, Klein M, Esdar C. M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models. Mol Cancer Ther. 2021 Aug;20(8):1378-1387. doi: 10.1158/1535-7163.MCT-21-0005. Epub 2021 May 27. PMID: 34045234.
4: Jenkins TW, Downey-Kopyscinski SL, Fields JL, Rahme GJ, Colley WC, Israel MA, Maksimenko AV, Fiering SN, Kisselev AF. Activity of immunoproteasome inhibitor ONX-0914 in acute lymphoblastic leukemia expressing MLL-AF4 fusion protein. Sci Rep. 2021 May 25;11(1):10883. doi: 10.1038/s41598-021-90451-9. PMID: 34035431; PMCID: PMC8149845.
