MNK/PIM-IN-2
MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC50 of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia.
For research use only. We do not sell to patients.
- CAS No.: 3081482-46-1
- Formula: C26H28FN7O2
- Molecular Weight:489.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
MNK/PIM-IN-2 (compound 2j) inhibits the proliferation of human leukemia cell lines MOLM-13, THP-1, U937 and K562 after 72 h[1].
MNK/PIM-IN-2 (1-2 μM; 12-24 h) induces G0/G1 phase arrest in human leukemia cell lines MOLM-13 and K562[1].
MNK/PIM-IN-2 (1-2 μM; 12-24 h) induces apoptosis in the human leukemia cell line MOLM-13, but exerts no significant apoptotic effect on the human leukemia cell line K562[1].
MNK/PIM-IN-2 (2 μM; 12-24 h) inhibits the Pim/Mnk signaling pathway in human leukemia cells MOLM-13 and K562, reduces the levels of p-eIF4E and p-4EBP1, downregulates the expression of Mcl-1 and c-Myc, and induces PARP cleavage in MOLM-13 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human leukemia cell lines (MOLM-13, THP-1, U937, K562)
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Concentration:/
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Incubation Time:72 h
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Result:Exhibited potent antiproliferative activity against MOLM-13 cells with a GI50 value of 0.19 μM.
Exhibited potent antiproliferative activity against THP-1 cells with a GI50 value of 1.04 μM.
Exhibited potent antiproliferative activity against U937 cells with a GI50 value of 0.59 μM.
Exhibited potent antiproliferative activity against K562 cells with a GI50 value of 0.70 μM.
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Cell Line:Human leukemia cell lines (MOLM-13, K562)
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Concentration:1, 2 μM
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Incubation Time:12 h (MOLM-13); 24 h (K562)
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Result:Induced G0/G1 phase arrest in MOLM-13 cells at 1 μM for 12 h, with 65.32% of cells in G0/G1.
Caused substantial accumulation in the sub-G1 phase in MOLM-13 cells at 2 μM for 12 h, with 40.44% of cells in sub-G1.
Induced G0/G1 phase arrest in K562 cells at 1 μM for 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb-c/nu (female) with subcutaneous MOLM‑13 cell inoculation to establish leukemia xenografts[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:daily; 2 weeks
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Result:Suppressed tumor growth with an inhibition rate of 57.1%.
Suppressed tumor growth with an inhibition rate of 72.6%.
Reduced Ki67 expression in tumor tissues.
Upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant changes in mouse body weight during administration.
Showed no abnormal changes in major organs via pathological analysis.
Chemical Information
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CAS No. 3081482-46-1
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Molecular Weight 489.54
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Formula C26H28FN7O2
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SMILES
FC1=CC(OC2CCOCC2)=C(NC3=C4C(C=CC(C5=CN(N=C5)C6CCNCC6)=N4)=NC=N3)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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