Biochem/physiol Actions

Reversible: yes

Primary TargetCXCR4

Cell permeable: yes

General description

A symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC₅₀ = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca²⁺ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC₅₀ = 200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC₅₀ = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kalatskaya, I., et al. 2009. Mol. Pharmacol.77, 1240.Pitchford, S.C., et al. 2009. Cell Stem Cell4, 62.De Clercq, E. 2009. Biochem. Pharmacol.77, 1655.Thoma, G., et al. 2008. J. Med. Chem.51, 7915. De Clercq, E. 2000. Mol. Pharmacol.57, 833.

Packaging

Packaged under inert gas

15 mg in Glass bottle

Physical form

A 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.

Warning

Toxicity: Standard Handling (A)