2. MAPK/ERK Pathway JAK/STAT Signaling Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. MNK Pim Apoptosis Caspase Eukaryotic Initiation Factor (eIF) PARP c-Myc
  4. 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.

MNK/PIM-IN-2

MNK/PIM-IN-2 Chemical Structure

CAS No. : 3081482-46-1

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MNK/PIM-IN-2 Related Antibodies

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PIM1 PIM2 PIM3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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[1].

In Vitro

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.

MNK/PIM-IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human leukemia cell lines (MOLM-13, THP-1, U937, K562)
Concentration: /
Incubation Time: 72 h
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.

Cell Cycle Analysis[1]

Cell Line: Human leukemia cell lines (MOLM-13, K562)
Concentration: 1, 2 μM
Incubation Time: 12 h (MOLM-13); 24 h (K562)
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.
Parmacokinetics
Species Dose Route Cmax T1/2 AUC0-last Bioavailability
Rat[1] 2 mg/kg i.v. 247 ng/mL 5.23 h 500 ng·h/mL /
Rat[1] 10 mg/kg i.p. 357 ng/mL 5.36 h 2235 ng·h/mL 90.31 %
In Vivo

MNK/PIM-IN-2 (10-20 mg/kg for 2 consecutive weeks) exhibits potent in vivo antileukemic activity in the MOLM-13 xenograft model, with no acute toxicity observed[1].

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

Animal Model: Balb-c/nu (female) with subcutaneous MOLM‑13 cell inoculation to establish leukemia xenografts[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: daily; 2 weeks
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.
Molecular Weight

489.54

Formula

C26H28FN7O2
CAS No.
SMILES

FC1=CC(OC2CCOCC2)=C(NC3=C4C(C=CC(C5=CN(N=C5)C6CCNCC6)=N4)=NC=N3)C=C1
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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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MNK/PIM-IN-2 Related Classifications

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  • 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:

MNK/PIM-IN-23081482-46-1MNKPimApoptosisCaspaseEukaryotic Initiation Factor (eIF)PARPc-MycMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinasePim kinasespoly ADP ribose polymerase MycMnk1Mnk2U937K562Pim1leukemia cellsCLK1THP-1MOLM-13CLK4Inhibitorinhibitorinhibit

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