PTPRO-IN-1
PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC50 of 0.16 μM. PTPRO-IN-1 exhibits IC50 values of 2.4 μM, 2.33 μM and 2.13 μM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-κB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C36H24ClNO6S
- Peso molecular:634.10
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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TLR4 |
IL-6 |
PTPRO-IN-1 (Compound 30k) (5 μM; 30 h) dose-dependently inhibits LPS (HY-D1056)-induced p-p65 expression and IL-6 secretion, as well as upregulation of TLR4 and phosphorylation of IKKα/β, in murine RAW264.7 and human THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated Raw 264.7 cells and THP-1-derived macrophages
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Concentration:5 μM
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Incubation Time:24 hours, followed by 1 μg/mL LPS stimulation for 4 hours
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Result:Dose-dependently inhibited LPS-induced p-p65 and IL-6 secretion.
Inhibited TLR4 upregulation and phosphorylation of IKKα/β.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male C57BL/6J mice (6-8 weeks
old)[1] -
Dosage:20 mg/kg
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Administration:i.g.; once daily for 10 days
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Result:Significantly reversed intestinal shortening and alleviated histological inflammation.
Significantly down-regulated the secretion of IFN-γ and IL-2 in CD4⁺/CD8⁺ T cells.
Chemical Information
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Peso molecular 634.10
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Fòrmula C36H24ClNO6S
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SMILES
OC1=CC=C(C#CC2=CC=C(C=C2)N(S(C3=CC=C4OC(C(O)=O)=CC4=C3)(=O)=O)CC5=CC=C(C=C5)C6=CC(Cl)=CC=C6)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PTPRO-IN-1 Related Classifications
HY-183573 Related Classifications
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