Shopping Cart

Your shopping cart is currently empty

M3258 (Synonyms: LMP7-IN-1)

Name: M3258
Brand: TargetMol
SKU: T11924
Price: 488 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T11924 Copy Product Info

Purity: 99.91%

🥰Excellent

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.

M3258

Copy Product Info

🥰Excellent

Catalog No. T11924

Synonyms LMP7-IN-1

Cas No. 2285330-15-4

Customer service consultation

Pack Size	Price	USA Stock	Global Stock
1 mg	$129	-	In Stock
5 mg	$322	-	In Stock
10 mg	$488	-	In Stock
25 mg	Preferential	-	In Stock
1 mL x 10 mM (in DMSO)	$232	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Cart

Add to Quotation

Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Batch Information

Select Batch

Purity:99.91%

ee:100%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS CNMR ORP CSFC

Product Introduction

Bioactivity

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.
Targets&IC50	LMP7:2–37 nM
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].
Synonyms	LMP7-IN-1

Chemical Properties

Molecular Weight	329.16
Formula	C₁₇H₂₀BNO₅
Cas No.	2285330-15-4
Smiles	C([C@H](NC(=O)[C@H]1[C@]2(O[C@@](C1)(CC2)[H])[H])B(O)O)C=3C=4C(OC3)=CC=CC4
Relative Density.	1.328 g/cm3 (Predicted)

Storage & Solubility Information

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.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (10.03 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0380 mL	15.1902 mL	30.3804 mL	151.9018 mL
5 mM	0.6076 mL	3.0380 mL	6.0761 mL	30.3804 mL
10 mM	0.3038 mL	1.5190 mL	3.0380 mL	15.1902 mL
20 mM	0.1519 mL	0.7595 mL	1.5190 mL	7.5951 mL
50 mM	0.0608 mL	0.3038 mL	0.6076 mL	3.0380 mL
100 mM	0.0304 mL	0.1519 mL	0.3038 mL	1.5190 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc