DPTIP (hydrochloride)

DPTIP is an inhibitor of neutral sphingomyelinase 2 (nSMase2; IC₅₀ = 30 nM).¹ It is selective for nSMase2 over alkaline phosphatase (ALP) and acid sphingomyelinase (IC₅₀s = >100 µM for both). DPTIP reduces viral yield in Vero and HeLa cells infected with West Nile virus (EC₅₀s = 0.26 and 2.81 µM, respectively) or Zika virus (EC₅₀s = 1.56 and 1.84 µM, respectively).² It inhibits the secretion of extracellular vesicles from primary mouse astrocytes activated by FBS withdrawal in a concentration-dependent manner and prevents serum deprivation-induced astrocyte activation in primary rat astrocytes when used at a concentration of 10 µM.¹ DPTIP (10 mg/kg) reduces IL-1β-induced extracellular vesicle release from astrocytes and decreases neutrophil infiltration to the brain in a model of inflammation-induced brain injury using GFAP-GFP mice. It reduces hepatic levels of chemokine (C-C motif) ligand 2 (Ccl2), Tnf-α, Il-6, and Il-1β in the same model.

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1. Rojas, C., Barnaeva, E., Thomas, A.G., et al. DPTIP, a newly identified potent brain penetrant neutral sphingomyelinase 2 inhibitor, regulates astrocyte-peripheral immune communication following brain inflammation. Sci. Rep. 8, 17715 (2018).

2. Álvarez-Fernández, H., Mingo-Casas, P., Blázquez, A.B., et al. Allosteric inhibition of neutral sphingomyelinase 2 (nSMase2) by DPTIP: From antiflaviviral activity to deciphering its binding site through in silico studies and experimental validation. Int. J. Mol. Sci. 23(22), 13935 (2022).