TRPM2 Inhibitor

JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia.

TAT-M2NX (tatM2NX) is a selective inhibitor targeting human TRPM2 channels and exerts inhibitory effects on ischemic stroke. TAT-M2NX reduces H₂O₂-induced calcium influx via TRPM2 channels. After traumatic brain injury in mice, TAT-M2NX preserves hippocampal long-term potentiation, improves memory function, and reduces infarct volume after middle cerebral artery occlusion, but it shows no effect on female mice. TAT-M2NX can be used in studies related to traumatic brain injury and ischemic stroke.

ZA10 is a selective TRPM2 channel inhibitor, with an IC₅₀ value of 8.1 μM. ZA10 can effectively suppress intracellular Ca²⁺ overload triggered by TRPM2 channel activation. ZA10 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA10 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC₅₀ = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC₅₀ >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research.