1. GPCR/G Protein MAPK/ERK Pathway
  2. Protease Activated Receptor (PAR) p38 MAPK
  3. 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.

For research use only. We do not sell to patients.

P2L-003

P2L-003 Chemical Structure

CAS No. : 1359416-20-8

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Description

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[1].

In Vitro

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.

Cell Viability Assay[1]

Cell Line: HT-29 cells
Concentration: 0, 10 and 30 μM
Incubation Time: 24 h
Result: Remained above 90 % even at the highest tested concentration of 30 μM.

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 3, 10 and 30 μM
Incubation Time: 24 h
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].
Molecular Weight

472.99

Formula

C23H25ClN4O3S

CAS No.
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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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P2L-003
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HY-180244
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