2. GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway
  3. Protease Activated Receptor (PAR) ERK
  4. I-287

I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.

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

I-287 Chemical Structure

I-287 Chemical Structure

CAS No. : 2014368-93-3

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Description

I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research[1].

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated activation of Gαq and Gα12/13 but not Gi/o proteins while has no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization[1].
I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated ERK1/2 activation in HEK293 cells[1].
I-287 (10 μM; 30 min) inhibits PAR2-induced secretion of IL-8 cytokine in HCT-116 and A549 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

I-287 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK-293 cells
Concentration: 0-60 μM
Incubation Time: 15 min
Result: Inhibited PAR2-mediated ERK1/2 activation in HEK293 cells.
In Vivo

I-287 (50 mg/kg for p.o.) reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CFA-induced paw inflammation in adult male C57BL/6J mice [1]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.) following the CFA
Result: Reduces CFA-induced inflammation in C57BL/6J mice
Molecular Weight

565.04

Formula

C30H30ClFN4O4
CAS No.
SMILES

O=C(C1=CN=C(N2CCN(C(C)(C2)C)C(C3=CC(N=C(C4=CC=C(C(F)=C4)Cl)C=C5C(C)(C)C)=C5O3)=O)C=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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I-287 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

I-2872014368-93-3I287I 287Protease Activated Receptor (PAR)ERKThrombin receptorsExtracellular signal regulated kinasesPAR2 inhibitorCFA-induced inflammationHEK-293ERK1/2GαqGα12/13Inhibitorinhibitorinhibit

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