2. MAPK/ERK Pathway
  3. MAPKAPK2 (MK2)
  4. MK2-IN-6

MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer.

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

MK2-IN-6 Chemical Structure

MK2-IN-6 Chemical Structure

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MK2-IN-6 Related Antibodies

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Description

MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer[1].

IC50 & Target

MK3

>100 nM (IC50)

FGFR4

>1000 nM (IC50)

TTK

>1000 nM (IC50)

p70S6Kb

>1000 nM (IC50)

MK5

>100 nM (IC50)

p38

>1000 nM (IC50)

In Vitro

MK2-IN-6 (2.3 nM, 70 min) exhibits high selectivity and irreversible inhibition on MK2, similar to PF-3644022 (HY-107427)[1].
MK2-IN-6 (1-10 μM, 1.5 or 6 h) profoundly suppresses cytokine transcription and production in macrophages, targeting classic downstream genes of MK2[1].

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

MK2-IN-6 Related Antibodies

Real Time qPCR[1]

Cell Line: Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
Concentration: 1-10 μM
Incubation Time: 6 h
Result: Effectively impeded the transcription and production of TNF-α, IL-6, and IL-1 increased by LPS in macrophages.

Western Blot Analysis[1]

Cell Line: Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
Concentration: 1-10 μM
Incubation Time: 1.5 h
Result: Significantly inhibited the phosphorylation of Hsp27 induced by LPS (100 ng/mL, 30 min) in macrophages, much more potent than that of PF-3644022 (HY-107427) and CC-99677 (HY-139504).
In Vivo

MK2-IN-6 (10 mg/kg, i.p., twice daily for 12 days) significantly hinders tumor growth in the MC38 tumor model of mice[1].

Pharmacokinetic parameters of MK2-IN-6 in the mouse[1]

药代动力学分析[1]

ip. (10 mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h·ng/mL) AUCinf_obc (h·ng/mL) MRTinf_obs (h)
Mean ± SD 0.38±0.034 0.05±0.00 125.87±46.0 44.49±21.4 45.19±21.3 1.64±2.08

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

Animal Model: MC38 tumor model of mice[1]
Dosage: 10 mg/kg
Administration: i.p., twice daily for 12 days
Result: The rates of tumor growth inhibition rates at dosages of 25 and 50 mg/kg MK2-IN-6 were 47.5% and 64.0%, respectively in MC38 tumor model of mice.
Molecular Weight

442.39

Formula

C22H17F3N4O3
SMILES

O=C(C=C)NC1=C(OC(F)(F)F)C=CC(C2=NC=CC(C3=CC(C(NCC4)=O)=C4N3)=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK2-IN-6 Related Classifications

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The dilution calculator equation

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

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

Keywords:

MK2-IN-6MAPKAPK2 (MK2)Mitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2MK2 inhibitorMK2 signalinginflammatory cytokinesmacrophagescolorectal cancerInhibitorinhibitorinhibit

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