STF-1084

STF-1084 is a cell-impermeable inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1, apparent Ki = 0. µM). It is selective for ENPP1 over ENPP2 and alkaline phosphatase (ALP, apparent Kis = 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. µM). It increases mRNA expression of the gene encoding IFN-beta 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.. Solulibility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml: Chloroform: Slightly Soluble: 0.1-1 mg/ml, DMSO: Slightly Soluble: 0.1-1 mg/ml, Methanol: Slightly Soluble: 0.1-1 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml.