IC50: 148 nM (TASK-1) and 1750 nM (TASK-3)[1]
TASK-1-IN-1 is a potent and selective TASK-1 (Potassium Channel) inhibitor with an IC50 of 148 nM. TASK-1-IN-1 shows a reduced inhibition of TASK-3 channels (IC50 of 1750 nM) and not a significant effect on other K+ channels. TASK-1-IN-1 has anticancer effects.
TASK-1-IN-1 (compound F3) blocks cell proliferation and viability in the MCF-7 cancer cell line but not in TASK-1 knockdown MCF-7 cells, indicating that it is acting in TASK-1 channels[1].
Cell Proliferation Assay[1]
| Cell Line: | MCF-7 cells |
| Concentration: | 10 μM |
| Incubation Time: | 96 hours |
| Result: | Showed an antiproliferative activity of ∼45% on the cell line MCF-7. |
[1]. BÁrbara ArÉvalo, et al. Selective TASK-1 Inhibitor with a Defined Structure-Activity Relationship Reduces Cancer Cell Proliferation and Viability. J Med Chem. 2022 Nov 24;65(22):15014-15027.