1. MAPK/ERK Pathway
  2. MAPKAPK2 (MK2)
  3. MK2-IN-3

MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo.

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MK2-IN-3 Chemical Structure

MK2-IN-3 Chemical Structure

CAS No. : 724711-21-1

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of MK2-IN-3:

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Description

MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo[1].

IC50 & Target

IC50: 8.5 nM (MK-2); 81 nM (MK-5); 210 nM (MK-3); 3.44 μM (ERK2); 5.7 μM (MNK1)[1]

In Vitro

MK2-IN-3 (compound 16) inhibits MK-2 and TNFα production in U937 cells, with IC50s of 8.5 nM and 4.4 μM, respectively[1].

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

In Vivo

MK2-IN-3 (compound 16) (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model[1].

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

Molecular Weight

340.38

Formula

C21H16N4O

CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C1C2=C(NC(C3=CC(C4=CC5=CC=CC=C5N=C4)=NC=C3)=C2)CCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (183.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9379 mL 14.6895 mL 29.3789 mL
5 mM 0.5876 mL 2.9379 mL 5.8758 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9379 mL 14.6895 mL 29.3789 mL 73.4473 mL
5 mM 0.5876 mL 2.9379 mL 5.8758 mL 14.6895 mL
10 mM 0.2938 mL 1.4689 mL 2.9379 mL 7.3447 mL
15 mM 0.1959 mL 0.9793 mL 1.9586 mL 4.8965 mL
20 mM 0.1469 mL 0.7345 mL 1.4689 mL 3.6724 mL
25 mM 0.1175 mL 0.5876 mL 1.1752 mL 2.9379 mL
30 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4482 mL
40 mM 0.0734 mL 0.3672 mL 0.7345 mL 1.8362 mL
50 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4689 mL
60 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
80 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9181 mL
100 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
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MK2-IN-3 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MK2-IN-3
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