Art. -Nr.: HY-12834

MK2-IN-1

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 0.11 uM for MK2 and an EC₅₀ of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein.

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Reinheit: 99.04%
CAS. Nr.: 1314118-92-7
Formel: C₂₇H₂₅ClN₄O₂
Molecular Weight:472.97

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MK2-IN-1 Chemical Structure

CAS. Nr.: 1314118-92-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Publications (6)
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Bioz

Biologische Aktivität

Beschreibung

Alle HSP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SW1353	CC₅₀	>20 μM Compound: 25	Cytotoxicity against human SW1353 cells after 30 mins by ATP-dependent luciferase luminescence assay Cytotoxicity against human SW1353 cells after 30 mins by ATP-dependent luciferase luminescence assay	[PMID: 24900358]
SW1353	EC₅₀	0.35 μM Compound: 25	Inhibition of MK2-mediated HSP27 phosphorylation in IL-1beta stimulated human SW1353 cells incubated for 30 mins prior to IL-1beta-stimulation measured after 27 mins by ELISA Inhibition of MK2-mediated HSP27 phosphorylation in IL-1beta stimulated human SW1353 cells incubated for 30 mins prior to IL-1beta-stimulation measured after 27 mins by ELISA	[PMID: 24900358]
SW1353	IC₅₀	5.7 μM Compound: 25	Inhibition of IL1beta-stimulated MMP13 secretion in human SW1353 cells incubated for 30 mins prior to IL1beta-stimulation measured after 24 hrs by ELISA Inhibition of IL1beta-stimulated MMP13 secretion in human SW1353 cells incubated for 30 mins prior to IL1beta-stimulation measured after 24 hrs by ELISA	[PMID: 24900358]
THP-1	EC₅₀	0.35 μM Compound: 1	Inhibition of MK2-mediated HSP27 phosphorylation at Ser78 in LPS-stimulated human THP-1 cells pre-incubated for 60 mins before LPS treatment measured after 60 mins Inhibition of MK2-mediated HSP27 phosphorylation at Ser78 in LPS-stimulated human THP-1 cells pre-incubated for 60 mins before LPS treatment measured after 60 mins	[PMID: 22182499]
THP-1	EC₅₀	350 nM Compound: 1	Inhibition of MK2 in human THP1 cells assessed as inhibition of LPS-induced HSP27 Ser78 phosphorylation incubated for 60 mins prior to LPS-induction measured after 60 mins Inhibition of MK2 in human THP1 cells assessed as inhibition of LPS-induced HSP27 Ser78 phosphorylation incubated for 60 mins prior to LPS-induction measured after 60 mins	[PMID: 24900435]
THP-1	EC₅₀	5 μM Compound: 2a	Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA	[PMID: 22169260]
THP-1	IC₅₀	4.4 μM Compound: 25	Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 30 mins prior to LPS-challenge measured after 3 hrs by ELISA Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 30 mins prior to LPS-challenge measured after 3 hrs by ELISA	[PMID: 24900358]
THP-1	IC₅₀	5.2 μM Compound: 25	Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 30 mins prior to LPS-challenge measured after 18 hrs by immunoabsorbent-based electrochemical luminescence assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 30 mins prior to LPS-challenge measured after 18 hrs by immunoabsorbent-based electrochemical luminescence assay	[PMID: 24900358]

In Vitro

MK2-IN-1 (purchased from MCE; 5 μM; 0.5-8 h) gradually increases Tfcp2l1 protein level without a change in the Tfcp2l1 transcript level within 2 h^[2].
MK2-IN-1 induces more alkaline phosphatase (AP)-positive colonies than the other factors in a short time^[2].

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

Western Blot Analysis^[2]

Cell Line:

46C mouse embryonic stem cells (mESCs)
Concentration:

5 μM
Incubation Time:

0.5, 1, 2, 8 h
Result:

The Tfcp2l1 protein level gradually increased without a change in the Tfcp2l1 transcript level within 2 h.

Chemical Information

CAS. Nr. 1314118-92-7
Appearance Solid
Molecular Weight 472.97
Formel C₂₇H₂₅ClN₄O₂
Color White to off-white
SMILES

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

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Journal Impact Factor

Nat Cell Biol

2026 Apr 24.
Cell Death Dis

Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]

2021 Oct 23;12(11):994. PMID: 34689152
Cell Rep

MK2 promotes Tfcp2l1 degradation via β-TrCP ubiquitin ligase to regulate mouse embryonic stem cell self-renewal. [Abstract]

2021 Nov 2;37(5):109949. PMID: 34731635
J Pharmacol Exp Ther

Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [Abstract]

2019 Aug;370(2):219-230. PMID: 31189728
Biol Pharm Bull

Stress Response Kinase MK2 Induces Non-canonical Activation of EphA2 in EML4-ALK Lung Cancer Cells. [Abstract]

2025;48(2):172-176. PMID: 40024717
University of Minnesota

2025.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Rao AU, et al. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72. [Content Brief]

[2]. Yan Zhang, et al. MK2 promotes Tfcp2l1 degradation via β-TrCP ubiquitin ligase to regulate mouse embryonic stem cell self-renewal. Cell Rep. 2021 Nov 2;37(5):109949. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MK2-IN-1

6 Cited Publications

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MK2-IN-1

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) MK2-IN-1

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MK2-IN-1

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) MK2-IN-1

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

MK2-IN-1 Related Classifications

HY-12834 Related Classifications