TNP

TNP is a cell-permeable inhibitor of inositol-1,4,5-trisphosphate 6-kinase 1 (IP₆K1; IC₅₀ = 0.55 µM; K_i = 0.24 µM) and IP₃K (IC₅₀ = 10.2 µM; K_i = 4.3 µM) that binds to the ATP-binding sites of both enzymes. ^1,2 TNP reduces IP₇ and IP₈ levels (IC₅₀s = ~3 and 1 µM, respectively) and inhibits insulin release in MIN6 cells.¹ It increases intracellular calcium levels in a concentration-dependent manner in HL-60 cells, potentially due to a 2- to 3-fold accumulation of IP₃, and induces degranulation in mast cells.³

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1. Padmanabhan, U., Dollins, D.E., Fridy, P.C., et al. Characterization of a selective inhibitor of inositol hexakisphosphate kinases: Use in defining biological roles and metabolic relationships of inositol pyrophosphates. The Journal of Biological Chemisty 284(16), 10571-10582 (2009).

2. Chang, Y.-T., Choi, G., Bae, Y.-S., et al. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem 3(9), 897-901 (2002).

3. Stokes, A.J., Shimoda, L.M., Lee, J.W., et al. Fcε RI control of Ras via inositol (1,4,5) trisphosphate 3-kinase and inositol tetrakisphosphate. Cell Signal. 18(5), 640-651 (2006).

Zhou, Y., Mukherjee, S., Huang, D., et al. Development of novel IP6K inhibitors for the treatment of obesity and obesity-induced metabolic dysfunctions. J. Med. Chem. 65(9), 6869-6887 (2022).