- Wang, H.R. et al. (2011) ACS Chem. Biol. 6, 845.
- Alomone Labs ML133 hydrochloride blocks Kir2.1 channels expressed in HEK293 cells.Top: Representative Kir2.1 current traces before (blue) and after (red) application of 10 µM ML133 hydrochloride (#M-275), recorded in pH 8.5 (left) or pH 7.4 (right). Currents were evoked from a holding potential of 0 mV by a 500 ms step to -100 mV, followed by a 500 ms ramp from -100 mV to 100 mV.
Bottom: Corresponding time course of Kir2.1 current inhibition by 10 µM ML133 hydrochloride, as indicated (bar) in pH 8.5 (left) or pH 7.4 (right).
ML133 hydrochloride is a selective small molecule that acts as an inhibitor of Kir2 inward rectifier potassium channels. The compound blocks Kir2.1, Kir2.6, Kir2.2 and Kir2.3 and shows little or no effect on other Kir channels1. ML133 hydrochloride demonstrates IC50 values of 1.8, 2.8, 2.9 and 4.0 μM for Kir2.1, Kir2.6, Kir2.2 and Kir2.3, respectively at pH 7.41.
Kir channels are a family of membrane proteins that selectively control the permeation of K+ ions across cell membranes. These channels play an important role in establishing the resting membrane potential of excitable cells, regulating pacing in cardiomyocytes and neurons, regulating pancreatic insulin secretion and renal K+ transport2.
ML133 hydrochloride (#M-275) is a highly pure, synthetic, and biologically active compound.