Plerixafor
CXCR4 antagonist / Plerixafor is a highly selective CXCR4 antagonist (IC50 = 20-130 nM).1,2 Originally investigated as an HIV replication inhibitor.3 Plerixafor has been investigated for the treatment autoimmune diseases and various cancers.4 Clinically useful for the mobilization of hematopoietic stem cells in the treatment of blood cancers.
Biochemicals & reagents
155148-31-5
AMD 3100.00
1) Donzella, et al. (1998), AMD3100, A Small Molecule Inhibitor of HIV-1 Entry via the CXCR4 Co-Receptor; Nat. Med. 4 72 2) Hatse et al. (2002), Chemokine Receptor Inhibition by AMD3100 Is Strictly Confined to CXCR4; FEBS Lett. 527 255 3) Bridger et al. (1995), Synthesis and Structure-Activity Relationships of Phenylenebis(methylene)-linked Bis-Tetraazamacrocycles That Inhibit HIV Replication. Effects of Macrocyclic Ring Size and Substituents on the aromatic Linker; J. Med. Chem. 38 366 4) Wang et al. (2020), CXCR4 antagonist AMD3100 (plerixafor): from an impurity to a therapeutic agent; Pharmacol. Res. 159 105010
RT
TARGET: GPCR -- PATHWAY: Cytokine -- RESEARCH AREA: Immunology; Stem Cells -- DISEASE AREA: Inflammation; CancerInfectious Disease; Pain