For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I045630 |
| CAS Number | 1596362-29-6 |
| Synonyms | (3S)-N-[(2S)-1-(cyclohexylmethylamino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-(4-oxo-4-phenylbutanoyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide;hydrochloride |
| Molecular Formula | C33H45ClN6O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C33H44N6O4.ClH/c34-33(35)36-19-9-16-27(31(42)37-21-23-10-3-1-4-11-23)38-32(43)28-20-25-14-7-8-15-26(25)22-39(28)30(41)18-17-29(40)24-12-5-2-6-13-24;/h2,5-8,12-15,23,27-28H,1,3-4,9-11,16-22H2,(H,37,42)(H,38,43)(H4,34,35,36);1H/t27-,28-;/m0./s1 |
| InChIKey | XHGSJQNAEULTAR-DHBRAOIWSA-N |
| SMILES | C1CCC(CC1)CNC(=O)C(CCCN=C(N)N)NC(=O)C2CC3=CC=CC=C3CN2C(=O)CCC(=O)C4=CC=CC=C4.Cl |
| Reference | [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. |
