PIM1-IN-8
PIM1-IN-8 is a PIM1/p65 pathway inhibitor. PIM1-IN-8 suppresses the expression of α-SMA and collagen I in activated fibroblasts and blocks TGF-β induced migration. PIM1-IN-8 alleviates pulmonary fibrosis in a Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis mice model. PIM1-IN-8 can be used for the study of idiopathic pulmonary fibrosis (IPF).
For research use only. We do not sell to patients.
- Formula: C17H17NO4
- Molecular Weight:299.32
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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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Help & FAQs
Biological Activity
PIM1-IN-8 (Compound B6) (20-50 μM, 48 h) displays inhibitory activity in NIH-3 T3 cells induced by TGF-β (10 ng/mL) (IR = 91.2) and a high cell viability rate (VR = 99.7) in GES-1 cells[1].
PIM1-IN-8 (3.125-100 μM, 24-48 h) inhibits fibroblast activation and proliferation in NIH-3 T3 and Ges-1 cells at concentrations ≥ 50 μM[1].
PIM1-IN-8 (2.5-10 μM) significantly suppresses the expression of α-SMA and collagen I in NIH-3 T3 cells[1].
PIM1-IN-8 (2.5-10 μM, 24 h) blocks TGF-β induced migration in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NIH-3 T3 and Ges-1 cells
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Concentration:3.125, 6.25, 12.5, 25, 50, 100 μM
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Incubation Time:24, 48 h
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Result:Inhibited fibroblast activation and proliferation in NIH-3 T3 and Ges-1 cells.
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Cell Line:A549 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Blocked TGF-β induced migration in A549 cells
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lung fibrosis was induced in male C57BL/6 mice (8-10 weeks old, 18-22 g) using Bleomycin (BLM) at a dose of 3 mg/kg.[1]
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Dosage:10, 20, 40 mg/kg
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Administration:i.p. daily for 14 days
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Result:Did not show toxicity at 500 mg/kg oral administration in mice.
Alleviated lung structural damage, including alveolar space collapse, thickened alveolar septa, and substantial collagen deposition.
Inhibited the expression of collagen I and α-SMA.
Reduced the levels of P21 and P16 in the lung tissue of IPF mice treated to 0.42 and 0.65, respectively.
Reduced the levels of IL-1β, IL-6 and the phosphorylation of P65.
Increased the levels of IL-10.
Chemical Information
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Molecular Weight 299.32
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Formula C17H17NO4
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SMILES
O=C(NC1=CC(C(C)=O)=C(O)C=C1OC)C2=CC=CC(C)=C2
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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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