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MK2-IN-3

Name: MK2-IN-3
Brand: TargetMol
SKU: T9034
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9034Cas No. 724711-21-1

Alias MK2 Inhibitor III

MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis

MK2-IN-3

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Purity: 99.01%

Catalog No. T9034Alias MK2 Inhibitor IIICas No. 724711-21-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
5 mg	$74	In Stock	In Stock
10 mg	$119	In Stock	In Stock
25 mg	$247	In Stock	In Stock
50 mg	$389	In Stock	In Stock
100 mg	$562	In Stock	In Stock
200 mg	$767	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$55	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.01%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

MK2-IN-3 AI Summary

MK2-IN-3 is a multifunctional kinase inhibitor with notable bioactivities. It shows strong inhibitory activity against MK2, MK3, MK5, and ERK2, with IC50 values ranging from 8.5 to 3440.0 nM but has lower activity against MNK1 and TNFalpha production in U937 cells and poor activity against kinases such as p38alpha, JNK2, IKK2, CDK2, MSK1, and MSK2 (IC50 values > 200,000 nM). In detailed bioactivity assays, it inhibits human recombinant MK2 with an IC50 of 8.5 nM and shows an EC50 of 49.0 nM. Further, it possesses a permeability of 6.0 nm/s by PAMPA and 5.0 nm/s across human Caco-2 cells, with a kinetic solubility of 0.0 μg/mL at pH 7.4. The compound has a short half-life in human (0.5833 hr) and rat (0.6667 hr) liver microsomes, with a high plasma protein binding of 99.7%. In an in vivo rat acute model of inflammation, MK2-IN-3 demonstrates a 20.0% inhibition at a 20 mg/kg dose one hour before an LPS challenge, though less effective (0.1%) when administered two hours prior. It also shows anti-inflammatory activity in human THP1 cells showing 38.0% inhibition of LPS-induced TNFalpha production at 10 µM. Overall, MK2-IN-3 demonstrates diverse kinase inhibitory activities, with particularly high potency against MK2, and a significant but varying anti-inflammatory effect..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis
Targets&IC50	MK3:210 nM (IC50), MK2:8.5 nM (IC50), MNK1:5.7 μM (IC50), ERK2:3.44 μM (IC50), MK5:81 nM (IC50)
Synonyms	MK2 Inhibitor III

Chemical Properties

Molecular Weight	340.38
Formula	C₂₁H₁₆N₄O
Cas No.	724711-21-1
Smiles	O=C1NCCc2[nH]c(cc12)-c1ccnc(c1)-c1cnc2ccccc2c1
Relative Density.	1.318 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: 9 mg/mL (26.44 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9379 mL	14.6895 mL	29.3789 mL	146.8946 mL
5 mM	0.5876 mL	2.9379 mL	5.8758 mL	29.3789 mL
10 mM	0.2938 mL	1.4689 mL	2.9379 mL	14.6895 mL
20 mM	0.1469 mL	0.7345 mL	1.4689 mL	7.3447 mL

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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