TASK-1-IN-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[1].

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

IC50: 148 nM (TASK-1) and 1750 nM (TASK-3)[1]

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.