ica-1

ICA-105665 (PF-04895162) is a potent and orally active opener of neuronal Kv7.2 7.3 and Kv7.3 7.5 potassium channels. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects [1][2][3][4].

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

ICA-105574 (ICA) is an activator of hERG that binds to the channel to remove inactivation, thus increasing peak current amplitude and shortening the action potential. It also modulates activation kinetics of the channel.

CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.

Sulcardine, a multi-ion channel blocker, reduces I Na and I Ca with IC 50 values of 26.9 µmol L and 69.2 µmol L, respectively. It has anti-arrhythmic effects [1].

dl-threo-2-methylisocitrate is a substrate of isocitrate lyase 1 (ICL1). IC50 value: target: using michael-menten nonlinear least squares fitting to determine the purified recombinant ICL1's Km for threo-D(s)L(s)-isocitrate (ICA) is 188°M and kcat is 5.24

MMPI-1154 is a highly promising imidazole-carboxylic acid (ICA) MMP-2 inhibitor (IC 50 = 6.6 μM) with excellent cardio-cytoprotective properties. It is specifically designed for the study of acute myocardial infarction. Additionally, MMPI-1154 exhibits significant inhibitory effects on MMP-13, MMP-1, and MMP-9 activities with IC 50 values of 1.8 μM, 10 μM, and 13 μM, respectively.

DL-threo-2-methylisocitrate is a substrate of isocitrate lyase 1 (ICL1). Using Michaelis-Menten nonlinear least squares fitting, the kcat value was 1.25 s-1 and the Km was 718 μM. In comparison, the Km of threonine-D(s)L(s)-isocitrate (ICA) was 188 μM and the kcat was 5.24 s-1.