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M3258
$282 – $2,250
Products Details
Product 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].
Web ID
– HY-111790
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C17H20BNO5
References
– [1]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.|[2]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.
CAS Number
– 2285330-15-4
Molecular Weight
– 329.16
Compound Purity
– 98.0
SMILES
– O=C(N[C@@H](CC1=COC2=C1C=CC=C2)B(O)O)[C@H]3[C@@H]4CC[C@@H](O4)C3
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 250 mg/mL (ultrasonic)
Target
– Apoptosis;Proteasome
Pathway
– Apoptosis;Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
