AJ2-30 is a specific small molecule SLC15A4 inhibitor with IFN-α suppression IC50 of 1.8  µM and MDP transport inhibition IC50 of 2.6  µM.
AJ2-30 shows no activity against a related family member, SLC15A3.
AJ2-30 displays similar activity against murine Slc15a4-mediated NOD2 activation.
AJ2-30 also blocks R848-induced activation of TLR7/8 signaling as well as TriDAP-induced and MDP-induced activation of NOD1 and NOD2 signaling, respectively, in THP-1 reporter cells.
AJ2-30 (10 uM) inhibites TLR7/8-induced production of TNF-α in human monocytes, also suppresses MDP-mediated and TriDAP-mediated TNF-α production in human macrophages, displays cross-species reactivity, suppressing IFN-α production in mouse pDCs.
AJ2-30 suppresses TLR7-9 and NOD activation of mouse immune cells in an Slc15a4-dependent manner.
AJ2-30 induces lysosomal-mediated degradation of SLC15A4.
AJ2-30 reduces inflammation in lupus patient cells and mice, suppresses inflammatory cytokine production in lupus patient-derived PBMCs.