Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

CXCR4:44 nM, CXCL12:5.7 nM

Plerixafor以略优于其对CXCR4亲和力的效力，抑制了CXCL12介导的趋化作用。[1] Plerixafor还以IC50为651 nM对SDF-1/CXCL12配体结合产生拮抗作用。对于SDF-1介导的GTP结合、SDF-1介导的钙流和SDF-1刺激的趋化作用，Plerixafor的IC50分别为27 nM、572 nM和51 nM。Plerixafor不抑制表达CXCR3、CCR1、CCR2b、CCR4、CCR5或CCR7的细胞在其相应配体刺激下的钙流，也不抑制LTB4的受体结合。Plerixafor本身不在表达多种GPCRs（包括CXCR4、CCR4和CCR7）的CCRF-CEM细胞中诱导钙流。[2]

单次局部施用Plerixafor能通过增加细胞因子产生、动员骨髓EPCs、增强成纤维细胞和单核细胞/巨噬细胞的活性，从而促进糖尿病小鼠的伤口愈合，同时增加血管生成和血管形成。[3] 小鼠连续五天被给予PBS、IGF1、PDGF、SCF或VEGF，并在第5天给予Plerixafor。与PDGF、SCF和VEGF处理组相比，IGF1加Plerixafor注射的小鼠群体中，克隆的数量和大小最大。[4]

In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively.

Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2]. U87 mg cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous "Treatments" section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2].