STF-1084

STF-1084 is a cell-impermeable inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1; apparent K_i = 0.11 µM).¹ It is selective for ENPP1 over ENPP2 and alkaline phosphatase (ALP; apparent K_is = 5.5 and >100 µM, respectively) and a panel of 468 kinases at 1 µM. STF-1084 inhibits the extracellular degradation of cGAMP in ENPP1-overexpressing and cGAS-expressing 293T cells (IC₅₀ = 0.340 µM). It increases mRNA expression of the gene encoding IFN-β in CD14⁺ primary human peripheral blood mononuclear cells (PBMCs) incubated with conditioned medium from ENPP1-overexpressing and cGAS-expressing 293T cells cultured with STF-1084. In vivo, STF-1084, in combination with ionizing radiation, increases the percentage of tumor-associated CD11c⁺ cells among antigen-presenting cells (APCs) in a 4T1 murine mammary cancer model.

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1. Carozza, J.A., Böhnert, V., Nguyen, K.C., et al. Extracellular cGAMP is a cancer-cell-produced immunotransmitter involved in radiation-induced anticancer immunity. Nat. Cancer 1(2), 184-196 (2020).