2. MAPK/ERK Pathway Apoptosis
  3. MNK Bcl-2 Family
  4. MNK1/2-IN-11

MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1 IC50 of 1.2 nM, MNK2 IC50 of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer.

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

MNK1/2-IN-11

MNK1/2-IN-11 Chemical Structure

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MNK1/2-IN-11 Related Antibodies

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Description

MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1 IC50 of 1.2 nM, MNK2 IC50 of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

MNK1

1.2 nM (IC50)

MNK2

1.3 nM (IC50)

Mcl-1

 

In Vitro

MNK1/2-IN-11 (compound 34) (72 h) inhibits the proliferation of CT26, HCT116, A549, MDA-MB-231, and LNCaP solid tumor cell lines with IC50 valuesof 11.7, 18.8, 13.0, 26.6 and 19.6 μM[1].
MNK1/2-IN-11 (1.25-5 μM; 3 days) dose-dependently inhibits eIF4E phosphorylation and reduces Mcl-1 and Cyclin D1 expression in CT26 colorectal cancer cells without affecting total eIF4E, MNK1, or Bcl-2 levels[1].
MNK1/2-IN-11 (1 μM) exhibits high kinase selectivity, with significant inhibition limited primarily to MNK1 and MNK2 at 1 μM, and only moderate inhibition of PIM1/3, JNK1/2/3, NEK1, and MET[1].

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

MNK1/2-IN-11 Related Antibodies

Western Blot Analysis[1]

Cell Line: CT26
Concentration: 1.25; 2.5; 5; 10 μM
Incubation Time: 3 days
Result: Dose-dependently inhibited phosphorylation of eIF4E at Ser209.
Suppressed the expression of downstream oncoproteins Mcl-1 and Cyclin D1.
Did not alter total eIF4E, MNK1, or Bcl-2 protein levels.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t F
Rat[1] 1 mg/kg i.v. 5.4 h 0.083 h 1454.7 ng/mL 1225.5 ng·h/mL /
Rat[1] 10 mg/kg p.o. 7.0 h 4 h 638.3 ng/mL 7616.9 ng·h/mL 62.2 %
In Vivo

MNK1/2-IN-11 (Compound 34) (50 mg/kg; p.o.; every other day; 14 days) inhibits tumor growth in a CT26 colorectal cancer mouse model[1].

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

Animal Model: Female Balb/c mice (5-6 weeks old) subcutaneously injected with CT26 cells[1]
Dosage: 50 mg/kg
Administration: p.o.; every other day; 14 days
Result: Achieved 36% tumor growth inhibition (TGI).
Combined with anti-mPD-1 antibody achieved 76% TGI.
Markedly augmented CD8+ T cell infiltration compared to monotherapy.
Caused no significant body weight loss.
Molecular Weight

537.61

Formula

C30H31N7O3
SMILES

O=C(C1=CC=C(C2=NN3C(C=C2)=NC=C3C(O4)=CC5=C4C=CN=C5N6C[C@H](N(C)C)CC6)C=C1)N7CCOCC7
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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MNK1/2-IN-11 Related Classifications

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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:

MNK1/2-IN-11MNKBcl-2 FamilyMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasecolorectal tumor modelsMNK1CT26eukaryotic translation initiation factor 4EHCT116anti-mPD-1 antibodyCD8+ T cellMNK2Mcl-1Cyclin D1Inhibitorinhibitorinhibit

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