| Name | M3258 |
| Description | M3258 is an immunoproteasome subunit LMP7 (β5i) inhibitor, with an IC50 of 3.6 nM for LMP7 and 3.4 nM at the cellular level. In a multiple myeloma xenograft model, M3258 exhibits significant antitumor activity. In multiple myeloma cells, M3258 significantly and persistently inhibits LMP7 activity and ubiquitinated protein turnover in tumor tissues, further inducing apoptosis. |
| In vitro | M3258 inhibits human LMP7 with an IC50 of 4.1 nM, while showing much weaker inhibitory activity against the constitutive proteasome subunit β5, with an average IC50 of 2519 nM.It also effectively inhibits LMP7 activity in human multiple myeloma cell lines MM.1S and U266B1, as well as in human, rat, and canine peripheral blood mononuclear cells (PBMCs), with IC50 values ranging from 2 to 37 nM.
In MM.1S cells, M3258 increases ubiquitinated protein levels by more than 4-fold, with an EC50 of 1980 nM, indicating that the compound disrupts the normal function of the immunoproteasome.Furthermore, M3258 induces apoptosis by activating caspase-3/7 activity, with an EC50 of 420 nM and an apoptosis induction fold of over 3.5. It also significantly reduces the viability of MM.1S cells, with an IC50 of 367 nM [2]. |
| In vivo | M3258 exhibits superior antitumor efficacy compared to the marketed non-selective proteasome inhibitors bortezomib and ixazomib in specific multiple myeloma and mantle cell lymphoma xenograft models at doses of 1 mg/kg and 10 mg/kg [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 200 mg/mL (607.61 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (10.03 mM), Sonication is recommended.
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| Keywords | M-3258 | M 3258 | LMP7 |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
United States
