PIM-IN-7
PIM-IN-7 is an orally active PIM inhibitor. PIM-IN-7 inhibits PIM-1 serine/threonine kinase activity as well as PIM-2, PIM-3, DYRK1A, and ERK7 kinase activities, with IC50 values of 6.71 nM, 15.14 nM, 10.10 nM, 48.18 nM, and 13.94 nM, respectively. PIM-IN-7 induces apoptosis, PARP cleavage, and G2/M cell cycle arrest, and reduces phosphorylation of the PIM substrates BAD, 4EBP1, and S6. PIM-IN-7 can be used for research on acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C19H20FN5O
- Molecular Weight:353.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PIM1 6.71 nM (IC50) |
PIM2 15.14 nM (IC50) |
PIM3 1010 nM (IC50) |
DYRK1A 48.18 nM (IC50) |
ERK7 13.94 nM (IC50) |
PARP |
4EBP1 |
S6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
0.21 μM
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Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
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acs.jmedchem.6c02920 |
| MOLM-13 | IC50 |
7.19 μM
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Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
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acs.jmedchem.6c02920 |
| RPMI-8226 | IC50 |
1.87 μM
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Antiproliferative activity against human RPMI 8226 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
Antiproliferative activity against human RPMI 8226 cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
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acs.jmedchem.6c02920 |
| MM1.S | IC50 |
11.06 μM
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Antiproliferative activity against human MM.1S cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
Antiproliferative activity against human MM.1S cells assessed as viability reduction incubated 96 hrs by CellTiter-Lumi luminescent assay.
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acs.jmedchem.6c02920 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, and 1 μM
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Incubation Time:48 h
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Result:Induced apoptosis in MV4-11 cells in a concentration-dependent manner.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, and 1 μM
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Incubation Time:48 h
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Result:At 0.1 μM, G1 was 55.09%, S was 29.45%, and G2/M was 15.46%; at 0.3 μM, G1 was 54.83%, S was 27.64%, and G2/M was 17.53%; at 1 μM, G1 was 29.39%, S was 18.11%, and G2/M was 52.50%.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, and 1 μM
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Incubation Time:48 h
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Result:Cleaved PARP was observed at 0.1 μM and increased markedly at 0.3 and 1 μM.
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Cell Line:MV4-11 cells
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Concentration:0.1, 0.3, 1, 3, 5, 7, and 10 μM
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Incubation Time:48 h
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Result:Phosphorylation of BAD (Ser122), 4EBP1 (Ser65), and S6 (Ser240/244) was reduced in a dose-dependent manner; total BAD, 4EBP1, and S6 levels remained unchanged.
Inhibition was detectable at 0.1 μM and became more pronounced at higher concentrations.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old)[1]
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Dosage:50 mg/kg; 25 mg/kg
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Administration:p.o.; once daily; 21 consecutive days
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Result:In the MV4-11 xenograft model, tumor growth inhibition (TGI) was 84.7% at 50 mg/kg once daily and 43.1% at 25 mg/kg once daily.
H&E staining showed necrosis in MV4-11 tumor tissues.
Western blot analysis of tumor lysates showed that PARP cleavage markedly increased relative to vehicle control.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
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Molecular Weight 353.39
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Formula C19H20FN5O
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SMILES
O=C1N[C@H](C)C2=C1C=C(C3=NC(C4=CN(C(C)(C)C)N=C4)=C(F)C=C3)N2
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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)
PIM-IN-7 Related Classifications
HY-191368 Related Classifications
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Keywords
- PIM-IN-7
- Pim
- DYRK
- ERK
- PARP
- Apoptosis
- Pim kinases
- Dual specificity tyrosine phosphorylation regulated kinase
- Dual specificity tyrosine regulated kinase
- Extracellular signal regulated kinases
- poly ADP ribose polymerase
- DYRK1A
- ERK7
- G2/M phase cell-cycle arrest
- MV4-11 xenograft
- PARP cleavage
- PIM-1 serine/threonine kinase
- PIM-2
- PIM-3
- acute myeloid leukemia
- apoptosis
- Inhibitor
- inhibitor
- inhibit