Icilin
TRPM8 inhibitor / Icilin is an agonist of cold-sensitive TRP channels with 2.5-fold greater efficacy and 200-fold greater potency than menthol (EC50 = 0.36 µM for CRM1, rat orthologue of TRPM8).1 Agonist at TRPM8 (EC50 = 0.2 µM)2 and ANKTM1(TRPA1)3. Agonist effects require Ca2+ and are pH dependent.2,4 Icilin induced G1 arrest in PC-3 prostate cancer cells without cell death.5
Biochemicals & reagents
36945-98-9
AG 3-5
1) McKemy et al. (2002) Identification of a cold receptor reveals a general role for TRP channels in thermosensation. Nature 416 52 2) Andersson et al. (2004) TRPM8 activation by menthol, icilin and cold is differentially modulated by intracellular pH J.Neurosci. 24 5364 3) Story et al. (2003) ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures Cell 112 819 4) Chuang et al. (2004) The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel Neuron 43 859 5) Kim et al. (2011) Icilin induces G1 arrest through activating JNK and p38 kinase in a TRPM8-independent manner. Biochem.Biophys.Res.Commun. 406 30
-20°C
TARGET: Ion channel -- PATHWAY: Cell cycle; Cation channel -- RESEARCH AREA: Neuroscience