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M3258

CAT: 0804-HY-111790-01Size: 10 mM - 1 mLDry Ice: NoHazardous: No
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CAT#:0804-HY-111790-01Size:10 mM - 1 mL
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells[1][2].
CAS Number
2285330-15-4
UNSPSC
12352005
Target
Apoptosis; Proteasome
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/M-3258.html
Purity
98.0
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C(N[C@@H](CC1=COC2=C1C=CC=C2)B(O)O)[C@H]3[C@@H]4CC[C@@H](O4)C3
Molecular Formula
C17H20BNO5
Molecular Weight
329.16
References & Citations
[1]Klein M, et al. Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) [published online ahead of print, 2021 Jul 6]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00604.|[2]Sanderson MP, et al. M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models [published online ahead of print, 2021 May 27]. Mol Cancer Ther. 2021;10.1158/1535-7163.MCT-21-0005.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1

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CatalogName
465513M3258

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