| ML401 is a potent antagonist of GPR183 (IC50 = 1.03 nM), also known as EBI2 or Epstein-Barr virus-induced gene 2. ML401 inhibited 7α,25-dihydroxycholesterol-induced RS11846 cell chemotaxis, IC50=6 nM.1 GPR183 is a key chemotactic receptor guiding B cell localization to appropriate microenvironments for activation and differentiation.2 It also regulates the homeostasis, localization and immunological function of splenic dendritic cells.3 Oxysterols have been shown to be endogenous ligands for GPR183 with 7α,25-dihydroxycholesterol being the most potent (Kd=450 pM).4 |
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