CXCR4 antagonist 7

CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome[1].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> GPCR/G Protein >> CXCR

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> CXCR

CXCR4/CXCL12:9.3 nM (IC50)

CXCR4 antagonist 7 (PARA-B, 10 nM-1 μM, 20 h) inhibits CXCL12-induced GH4C1 cell proliferation with an IC50 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 IC50 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.

[1]. Rosa Maria Vitale, et al. Identification of the hydantoin alkaloids parazoanthines as novel CXCR4 antagonists by computational and in vitro functional characterization. Bioorg Chem. 2020 Dec;105:104337.