PS372424 hydrochloride

PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation[1][2].

Signaling Pathways >> GPCR/G Protein >> CXCR

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> CXCR

Human CXCR3

PS372424 (100 ng/mL) increases p-Erk1 and p-Erk2 in U87-CXCR3-A cells after 5 min of stimulation[1]. PS372424 (10-200 nM; 30 min) causes a concentration-dependent phosphorylation of CCR5 on CXCR3+ T cells not in CXCR3- T cells[2]. PS372424 competes for binding of radiolabeled CXCL10 to membranes prepared from HEK293/CXCR3 Gqi5 cells with an IC50 of 42±21 nM[3]. Western Blot Analysis[2] Cell Line: CXCR3+ T cells and CXCR3- T cells Concentration: 10, 50, 100, or 200 nM Incubation Time: 30 minutes Result: Caused a concentration-dependent phosphorylation of CCR5 on CXCR3+ T cells. Did not result in phosphorylation of CCR5 on CXCR3- T cells.

[1]. Boyé K, et al. The role of CXCR3/LRP1 cross-talk in the invasion of primary brain tumors. Nat Commun. 2017 Nov 17;8(1):1571.

[2]. O'Boyle G, et al. Chemokine receptor CXCR3 agonist prevents human T-cell migration in a humanized model of arthritic inflammation. Proc Natl Acad Sci U S A. 2012 Mar 20;109(12):4598-603.

[3]. Stroke IL, et al. Identification of CXCR3 receptor agonists in combinatorial small-molecule libraries. Biochem Biophys Res Commun. 2006 Oct 13;349(1):221-8.