1. Metabolic Enzyme/Protease
    Apoptosis
  2. Proteasome
    Apoptosis
  3. M3258

M3258 

Cat. No.: HY-111790 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

M3258 Chemical Structure

M3258 Chemical Structure

CAS No. : 2285330-15-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 282 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 282 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

LMP7[1]

In Vitro

M3258 inhibits human LMP7 with a mean IC50 of 4.1 nM. M3258 displays weak activity against the constitutive proteasome subunit β5 (mean IC50=2519 nM). M3258 potently inhibits LMP7 in the human multiple myeloma cell lines MM.1S and U266B1 and in human, rat, and dog PBMCs with IC50s between 2 and 37 nM[2].
M3258 induces a >four fold accumulation of ubiquitinated proteins with an EC50 of 1980 nM in MM.1S cells. M3258 interferes with immunoproteasome function. M3258 also induces apoptosis assessed by caspase 3/7 activity (EC50=420 nM;>3.5-fold induction) and reduces MM.1S cell viability (IC50=367 nM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: MM.1S cells
Concentration: 0.01-100 nM
Incubation Time: 2 hours
Result: Potently inhibited LMP7 in the human multiple myeloma cell lines MM.1S (IC50=2.2 nM).
In Vivo

M3258 (1 mg/kg; 10 mg/kg) shows superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female H2d Rag2 mice or female CB-17 SCID mice (U266B1 subcutaneous xenograft model; MM.1S subcutaneous xenograft model)[2]
Dosage: 1 mg/kg in U266B1 subcutaneous xenograft model; 10 mg/kg in MM.1S subcutaneous xenograft model
Administration: P.o.; either once daily, every 2 days or twice weekly (days 1 and 4)
Result: Displayed significant and strong antitumor efficacy.
Clinical Trial
Molecular Weight

329.16

Formula

C₁₇H₂₀BNO₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (759.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0380 mL 15.1902 mL 30.3804 mL
5 mM 0.6076 mL 3.0380 mL 6.0761 mL
10 mM 0.3038 mL 1.5190 mL 3.0380 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.32 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: ≥98.0%

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M3258
Cat. No.:
HY-111790
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