IQM-266 is a Downstream Regulatory Element Antagonist Modulator (DREAM) ligand with a K D of 4.63 μM. IQM-266 inhibits the K V 4.3 /DREAM current in a concentration-, voltage-, and time-dependent-manner. IQM-266 also modulates A-type outward potassium currents (IA) from rat dorsal root ganglia (DRG) neurons. IQM-266 can be used for neurological disease research, such as Alzheimer’s disease and Huntington's disease (HD) [1].
In Vitro, IQM-266 (0-100 μM) concentration-dependently inhibits Kv4.3/DREAM channels (IC50 = 8.6 μM) in CHO cells by slowing their activation and inactivation kinetics[1]. IQM-266 (0-100 μM) inhibits the maximum peak current and, to a lesser extent, the charge crossing the cell membrane during depolarization at ≥ 10 μM in CHO cells[1]. IQM-266 (3 μM) increases the charge through the cell membrane during the application of depolarizing pulses, and inhibits peak Kv4.3/DREAM current amplitude while slowing its inactivation in CHO cells[1]. IQM-266 (3-10 μM) slows the recovery process and increases closed-state inactivation of Kv4.3/DREAM channels in a concentration-dependent manner in CHO cells through its specific interaction with DREAM, which also underlies the observed increase in transmembrane charge[1]. IQM-266 (3-10 μM) dose-dependently reduces the peak amplitude of IA in rat DRG neurons[1].
References:
[1]. Peraza DA, et al. Identification of IQM-266, a Novel DREAM Ligand That Modulates KV4 Currents. Front Mol Neurosci. 2019 Feb 4;12:11.
In Vitro, IQM-266 (0-100 μM) concentration-dependently inhibits Kv4.3/DREAM channels (IC50 = 8.6 μM) in CHO cells by slowing their activation and inactivation kinetics[1]. IQM-266 (0-100 μM) inhibits the maximum peak current and, to a lesser extent, the charge crossing the cell membrane during depolarization at ≥ 10 μM in CHO cells[1]. IQM-266 (3 μM) increases the charge through the cell membrane during the application of depolarizing pulses, and inhibits peak Kv4.3/DREAM current amplitude while slowing its inactivation in CHO cells[1]. IQM-266 (3-10 μM) slows the recovery process and increases closed-state inactivation of Kv4.3/DREAM channels in a concentration-dependent manner in CHO cells through its specific interaction with DREAM, which also underlies the observed increase in transmembrane charge[1]. IQM-266 (3-10 μM) dose-dependently reduces the peak amplitude of IA in rat DRG neurons[1].
References:
[1]. Peraza DA, et al. Identification of IQM-266, a Novel DREAM Ligand That Modulates KV4 Currents. Front Mol Neurosci. 2019 Feb 4;12:11.