GPC-100 (TG-0054, Burixafor) is a novel small molecule antagonist of CXCR4, shows competitive inhibition of CXCL12 binding to CXCR4 with Ki of 1.6 nM. GPC-100 (TG-0054, Burixafor) demonstrates distinct divergence from AMD3100, and has a higher affinity for CXCR4 than AMD3100 (Ki=40 nM). GPC-100 (TG-0054, Burixafor) dose dependenlyt inhibits CXCL12-induced calcium flux in MDA-MB-231 cells overexpressing CXCR4 with IC50 value of 30 nM. GPC-100 (TG-0054, Burixafor) inhibits CXCL12 mediated recruitment of β-arrestin to CXCR4 with IC50 value of 207 nM in the PRESTO-TANGO β-arrestin assay. GPC-100 (TG-0054, Burixafor) efficiently blocks CXCL12-mediated migration in U937 and MM.1S cells with IC50 of 48 nM and 28 nM, respectively.
