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AMD3451 is a specific, dual CXCR5/CXCR4 antagonist with antiviral activity against a wide variety of HIV-1 and HIV-2 (IC50=1.2 to 26.5 uM) in vitro.AMD3451 has antiviral activity against a wide variety of R5, R5/X4, and X4 strains if HIV-1 and HIV-2 in various T-cell lines, CCR5- or CXCR4-transfected cells, PBMCs, and monocytes/macrophages.AMD3451 inhibited R5, R5/X4, and X4 HIV-1 primary clinical isolates in PBMCs (IC50, 1.8 to 7.3 uM), AMD3451 blocks R5 and X4 HIV-1 infection at the virus entry stage.AMD3451 dose-dependently inhibited the intracellular Ca2+ signaling induced by the CXCR4 ligand CXCL12 in T-lymphocytic cells and in CXCR4-transfected cells, as well as the Ca2+ flux induced by the CCR5 ligands CCL5, CCL3, and CCL4 in CCR5-transfected cells.AMD3451 did not interfere with chemokine-induced Ca2+ signaling through CCR1, CCR2, CCR3, CCR4, CCR6, CCR9, or CXCR3 and did not induce intracellular Ca2+ signaling by itself at 400 uM.AMD3451 inhibited CXCL12- and CCL3L1-induced endocytosis in CXCR4- and CCR5-transfected cells.AMD3451 does not inhibit the binding of CXCR4- or CCR5-specific MAbs.
YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.
alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.
PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.
RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.
SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.
ML 339 is a potent and selective hCXCR6 antagonist (IC50 = 140 nM), 100-fold less active at the murine CXCR6 receptor (IC50 = 18 uM);
ML 339 exhibits selectivity over CXCR5, CXCR4, CCR6 and APJ receptors.
CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor;
Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339.
CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.
CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.
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