Deltafluorine
Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma.
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- Formule: C33H42ClFN4O4S2
- Masse moléculaire:677.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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PDEδ 27 nM (IC50) |
PDEδ 148 nM (Kd) |
ERK1 |
ERK2 |
Deltafluorine (Compound 22a) (60 μM; 0-7 days) covalently modifies purified PDEδ at residue p.E88 with >85% efficiency over 7 days in vitro, with a second-order rate constant of 5.4 M−1 s−1[1].
Deltafluorine (10 μM; 2 h) induces significant thermal stabilization of PDEδ in Jurkat cells with a ΔTm of 16.6 ± 3.2 °C[1].
Deltafluorine (5 μM; 0.25-4 h) reduces phosphorylation of ERK1/2 and S6 in PA-TU-8902 cells[1].
Deltafluorine (5 μM; 0-120 h) inhibits the proliferation of PA-TU-8902 cells with 84 ± 2% growth inhibition[1].
Deltafluorine (5 μM; 2 h) inhibits the MAPK and Akt-mTOR pathways in PA-TU-8902 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PA-TU-8902 cells
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Concentration:5 μM
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Incubation Time:0.25, 0.5, 1, 2, 4 h
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Result:Reduced phosphorylation of ERK1/2 (Thr202/Tyr204) and S6 (S235/236) in PA-TU-8902 cells over the time course.
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Cell Line:PA-TU-8902 cells
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Concentration:5 μM
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Incubation Time:4 h treatment + 20 h wash-out regimen over 4 days
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Result:Inhibited growth of PA-TU-8902 cells with 84 ± 2% growth inhibition under wash-out conditions.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KrasLSL.G12D/wt; Trp53fl/fl (KP mice; autochthonous lung adenocarcinoma model induced by intratracheal Adeno-CMV-Cre instillation)[1]
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Dosage:15 mg/kg
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Administration:I.p.; daily; 21 days
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Result:Reduced tumor load by 42% compared to untreated controls.
Lowered lung tumor volume occupancy to 21.6% versus 47.5% in untreated controls.
Chemical Information
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Masse moléculaire 677.29
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Formule C33H42ClFN4O4S2
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SMILES
CC1=NC(C)=C(CF)C=C1CN(S(=O)(C2=CC=C(S(=O)(N(C3CCCC3)CC4=CC=C(Cl)C=C4)=O)C=C2)=O)CC5CCNCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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