CXCR4 antagonist 7 (Compound PARA-B) is able to be used in the HIV infection, inflammatory diseases, cancer, and WHIM syndrome research which is a antagonist of CXCR4 (IC 50 = 9.3 nM) [1].

CXCR4 antagonist 7 (PARA-B, 10 nM-1 μM, 20 h) inhibits CXCL12-induced GH4C1 cell proliferation with an IC 50 value of 9.3 nM [1]. CXCR4 antagonist 7 (1 μM, 12 h) inhibits CXCL12-dependent GH4C1 cell migration with inhibition rate of 50% [1]. CXCR4 antagonist 7 (50 nM, 30 min) reduces ERK1/2 phosphorylation induced by CXCL12 [1]. CXCR4 antagonist 7 (50 nM-1 μM, 30 min) acts via CXCR4 antagonism to revert CXCL12 induction of GH4C1 proliferation and migration [1]. Cell Viability Assay [1] Cell Line: GH4C1 cell (48 h of serum deprivation) Concentration: 1 μM Incubation Time: 24 h Result: Had no effect on cell viability of GH4C1 cell. Cell Proliferation Assay [1] Cell Line: GH4C1 cell ( FBS-starved GH4C1 cells treated with CXCL12 (25 nM) for 12 h) Concentration: 10 nM-1 μM Incubation Time: 20 h, 24 h Result: Inhibited proliferation of multiple cancer cell lines with IC 50 value ranging from 1.08 to 3.45 μM, and had no effect on cell viability of GH4C1cell. Cell Migration Assay [1] Cell Line: GH4C1 and GH4A11 cells (FBS-starved cells treated with CXCL12 (25 nM) for 48 h) Concentration: 50 nM-1 μM Incubation Time: 12 h for GH4C1, 30 min for GH4A11 Result: Reduced the number of migrating GH4C1 cells significantly, had no effect on GH4A11 cell (CRISPR-CAS9, reduction in CXCR4 mRNA) migration. Western Blot Analysis [1] Cell Line: GH4C1 cell (FBS-starved cells treated with CXCL12 (25 nM) for 15 min) Concentration: 50 nM Incubation Time: 30 min Result: Reduced ERK1/2 phosphorylation induced by CXCL12.