Table 1.
Test material | IC50 (nmol/L) | ||
---|---|---|---|
IP6K1 | IP6K2 | IP6K3 | |
SC-919 | <5.2a | <3.8a | 0.65 ± 0.13 |
TNP | 270 ± 100 | 850 ± 330 | 260 ± 21 |
The ADP-glo assay condition was performed as follow: The compounds were co-incubated with recombinant human IP6K1 (15 nM), human IP6K2 (12 nM), or human IP6K3 (1.5 nM) in the assay buffer. Following the addition of ATP and InsP6 at final concentrations of 15 and 50 μM, respectively, a kinase reaction was carried out for 2 h. Thereafter, the ADP-Glo™ kinase assay (Promega, Madison, WI, USA) was performed.
aSC-919 showed inhibitory activity reaching detection limits for IP6K1 assay and IP6K2 assay, respectively. Values indicate mean ± S.D. (n = 3 biological replicates of 4–8 technical replicates).