PS372424 

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

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].

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

588.74

C₃₃H₄₄N₆O₄

914291-61-5

Solid

White to off-white

O=C([C@H]1N(C(CCC(C2=CC=CC=C2)=O)=O)CC3=C(C=CC=C3)C1)N[C@H](C(NCC4CCCCC4)=O)CCCNC(N)=N

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]