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Plerixafor

Catalog No. T1776 CAS 110078-46-1

Synonyms: JM3100, AMD 3100, AMD-3329

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

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Plerixafor, CAS 110078-46-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 42.00
10 mg	In stock	$ 63.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 179.00
100 mg	In stock	$ 323.00
200 mg	In stock	$ 513.00
500 mg	In stock	$ 818.00

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Purity: 100%

Purity: 99.17%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.
Targets&IC50	CXCR4:44 nM, CXCL12:5.7 nM
In vitro	Plerixafor inhibits CXCL12-mediated chemotaxis with a potency lightly better than its affinity for CXCR4. [1] Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF–CEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7. [2]
In vivo	A single topical application of Plerixafor promotes wound healing in diabetic mice by increasing cytokine production, mobilizing bone marrow EPCs, and enhancing the activity of fibroblasts and monocytes/macrophages, thereby increasing both angiogenesis and vasculogenesis. [3] Cohorts of mice are administered with PBS, IGF1, PDGF, SCF, or VEGF for five consecutive days and Plerixafor on the 5th day. The number and size of the colonies are highest in IGF1 plus Plerixafor injected mice compared to PDGF, SCF and VEGF treated groups, in combination with Plerixafor. [4]
Kinase Assay	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.
Cell Research	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].

Synonyms	JM3100, AMD 3100, AMD-3329
Molecular Weight	502.78
Formula	C28H54N8
CAS No.	110078-46-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

PBS: 1 mg/mL (1.98 mM), Sonification is recommended.

Ethanol: 50 mg/mL, Sonification is recommended.

DMSO: 2 mM, Sonification is recommended.

H2O: Insoluble

References and Literature

1. Zabel BA, et al. J Immunol. 2009, 183(5), 3204-3211. 2. Fricker SP, et al. Biochem Pharmacol. 2006, 72(5), 588-596. 3. Nishimura Y, et al. J Invest Dermatol. 2012, 132(3 Pt 1), 711-720. 4. Kumar S, et al. Bone. 2012, 50(4), 12012-12018. 5. Wei He, et al. Targeting CXC motif chemokine receptor 4 inhibits the proliferation, migration and angiogenesis of lung cancer cells. Oncol Lett. 2018 Sep;16(3):3976-3982. 6. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. 7. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926. 8. He G, et al. SDF-1 in Mammary Fibroblasts of Bovine with Mastitis Induces EMT and Inflammatory Response of Epithelial Cells. Int J Biol Sci. 2017 May 5;13(5):604-614. 9. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Citations

1. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Viral Compound Library Bioactive Compounds Library Max GPCR Compound Library Human Metabolite Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Plerixafor 110078-46-1 Autophagy GPCR/G Protein Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease Virus Protease CXCR JM 3100 stream inhibit multiple Inhibitor SID-791 Human immunodeficiency virus cancer G-CSF human JM-3100 stem myeloma JM3100 SID 791 cells blood AMD 3100 CXC chemokine receptors lymphoma AMD3100 SID791 HIV ligand AMD 3329 AMD3329 AMD-3329 mobilizer peripheral AMD-3100 inhibitor

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