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.
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- Formel: C22H17F3N4O3
- Molecular Weight:442.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
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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.
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Cell Line:Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
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Concentration:1-10 μM
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Incubation Time:6 h
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Result:Effectively impeded the transcription and production of TNF-α, IL-6, and IL-1 increased by LPS in macrophages.
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Cell Line:Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
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Concentration:1-10 μM
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Incubation Time:1.5 h
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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
Pharmacokinetic parameters of MK2-IN-6 in the mouse[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 |