Plerixafor 8HCl (AMD3100 8HCl) is a potent and selective antagonist of CXCL12-mediated chemotaxis and G-protein coupled chemokine receptor (CXCR4) with IC50 values of 5.7 and 44 nM, respectively [1]. Plerixafor 8HCl has shown a high selectivity for CXCR4 compared other chemokine receptors including LTB4 CCR1, CCR2b, CCR4, CCR5, CCR7, CXCR3, etc [2].
Plerixafor 8HCl showed to inhibit I-SDF-1 ligand binding to CCRF–CEM T-lymphoblastoid cells which express CXCR4. Plerixafor 8HCl has shown to block CXCR4 activation, SDF-1 mediated calcium flux and SDF-1 mediated chemotaxis with IC50 values of 27.3, 572 and 51 nM, respectively [2].
References:
[1] Zabel BA1,?Wang Y,?Lewén S,?Berahovich RD,?Penfold ME,?Zhang P,?Powers J,?Summers BC,?Miao Z,?Zhao B,?Jalili A,?Janowska-Wieczorek A,?Jaen JC,?Schall TJ. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol.?2009 Sep 1;183(5):3204-11. doi: 10.4049/jimmunol.0900269. Epub 2009 Jul 29.
[2] Fricker SP1,?Anastassov V,?Cox J,?Darkes MC,?Grujic O,?Idzan SR,?Labrecque J,?Lau G,?Mosi RM,?Nelson KL,?Qin L,?Santucci Z,?Wong RS. Characterization?of the?molecular?pharmacology?of?AMD3100: a?specific?antagonist?of the?G-protein?coupledchemokine?receptor,?CXCR4. Biochem Pharmacol.?2006 Aug 28;72(5):588-96.
