A cell-permeable quinazoline compound that acts as a potent and reversible CXCR4 antagonist (IC50 = 36.2 nM for SDF-1/CXCL12 binding to hCXCR4-transfected HEK293 membrane) with selectivity over closely related human chemokine receptors CXCR2, CCR2, CCR4 and CCR5 (IC50 >10 µM). Shown to inhibit CXCL12-induced Ca2+-mobilization and cell migration in hCXCR4-HEK293 cells (IC50 = 100.1 and 41 nM, respectively), and rapidly mobilize CXCR4+, CD34+ and CD133+ stem cells from bone marrow in C57BL/6 male mice (6 mg/kg, s.c).
生物化学的/生理学的作用
Cell permeable: yes
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
再構成
Following reconstitution, aliquot and freeze (20°C). Stock solutions are stable for up to 6 months at -20°C.
その他情報
Wu, C.H., et al. 2012. Chem. Med. Chem.7, In press.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany