P2L-003
P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. P2L-003 blocks PAR2-mediated Ca2+ mobilization without affecting PAR1, PAR4, or ATP-mediated signaling and dose-dependently suppresses the downstream MAPK signaling cascades, including ERK1/2 and p38 phosphorylation. P2L-003 can be used for colon cancer research.
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- CAS. Nr.: 1359416-20-8
- Formel: C23H25ClN4O3S
- Molecular Weight:472.99
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
P2L-003 (0-30 μM, 24 h) does not compromise cell proliferation in HT-29 cells[1].
P2L-003 (3-30 μM, 24 h) not only blocks PAR2-mediated Ca2+ mobilization but also suppresses downstream ERK1/2 and p38 signaling cascades in a concentration-dependent manner in HT-29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:0, 10 and 30 μM
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Incubation Time:24 h
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Result:Remained above 90 % even at the highest tested concentration of 30 μM.
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Cell Line:HT-29 cells
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Concentration:3, 10 and 30 μM
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Incubation Time:24 h
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Result:Reduced the phosphorylation levels of both ERK1/2 and p38 relative to their total protein levels in a dose-dependent manner[1].
Inhibited PAR2-induced MAPK pathway activation[1].
Chemical Information
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CAS. Nr. 1359416-20-8
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Molecular Weight 472.99
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Formel C23H25ClN4O3S
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SMILES
ClC1=C(CS(N2CC(C(CN(C(C)=O)C3=CC=CC=C3)=NN4C)=C4CC2)(=O)=O)C=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)