1092776-63-0

IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC₅₀s = 8 and 11 nM for the human and rat receptors, respectively). It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/K_v11.1; IC₅₀ = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC₅₀ = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC₅₀ = 79.1 nM). It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC₅₀s = 14.2 and 19 nM, respectively). IT1t (20 μM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.

N,N''-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl Ester Dihydrochloride is a potent CXCR4 antagonist. It also exhibits anti-viral activity against HIV.

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[1]. thoma g, streiff mb, kovarik j, et al. orally bioavailable isothioureas block function of the chemokine receptor cxcr4 in vitro and in vivo. j med chem, 2008, 51(24): 7915-7920.