DDO3711
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.
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- CAS No.: 2673364-10-6
- Formule: C42H41N9O6
- Masse moléculaire:767.83
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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MAP3K6/ASK2 >20 μM (IC50) |
DDO3711 (15 μM; 24 h) shows antiproliferation effects on gastric cancer cells by reducing p-ASK1T838 in a PP5-dependent manner. DDO3711 does not inhibit the proliferation of GES-1 cells and HGC-27 cells[1].
DDO3711 (5 μM; 1-24 h) inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner[1].
DDO3711 (5-50 μM; 0.5-2 h) potently dephosphorylates p-ASK1T838 both in vitro and in cells. DDO3711 concentration-dependently reduced the level of p-JNK and p-p38[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN45 cells
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Concentration:15 μM
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Incubation Time:24 h
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Result:Showed strong antiproliferative activity (IC50=0.5 μM).
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Cell Line:MKN45 cells
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Concentration:5 μM
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Incubation Time:1-24 h
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Result:Inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner.
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Cell Line:MKN45 cells
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Concentration:5, 25, 50 μM
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Incubation Time:0.5-2 h
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Result:Could dephosphorylate p-ASK1T838 in a time- and concentration-dependent manner in vitro.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old BALB/c nude mice with MKN45 cells[1]
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Dosage:20, 40 mg/kg
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Administration:IP; daily; for 21 days
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Result:Caused significant inhibition of tumor growth in a dose-dependent manner.
Significantly decreased the level of p-ASK1T838.
Chemical Information
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CAS No. 2673364-10-6
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Masse moléculaire 767.83
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Formule C42H41N9O6
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SMILES
COC1=CC=C(C=C1OC)C2=NC(CC3=CC=C(C=C3)C(NCCCCCCNC(C4=CC=C(C=C4)C(NC5=CN6C=C(C=CC6=N5)N7C=CN=C7)=O)=O)=O)=NO2
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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)
DDO3711 Related Classifications
HY-152247 Related Classifications
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