AE 51310
OPN4/Melanopsin antagonist / AE 51310 is a potent antagonist of the GPCR OPN4/melanopsin (Ki = 0.096 nM human OPN4).1 OPN4 regulates circadian rhythms, pupil functions, melatonin expression, cognition, and sleep. OPN4 has been found to bind Gα11 in lung cancer cells modulating PKC activation leading to activation of BRAF/MEK/ERK signaling pathways. AE 51310 decreased the growth and proliferation of both LG17 and LG55 lung cancer tumors in mouse xenograft models.
Biochemicals & reagents
433966-92-8
1) Jones et al. (2013), Small-molecule antagonists of melanopsin-mediated phototransduction; Nat. Chem. Biol. 9 630 2) Wang et al. (2020), Targeting Opsin4/Melanopsin with a Novel Small Molecule Suppresses PKC/RAF/MEK/ERK Signaling and Inhibits Lung Adenocarcinoma Progression; Mol. Cancer Res. 18 1028
-20°C
TARGET: OPN4/Melanopsin antagonist -- PATHWAY: Proliferation; ERK -- RESEARCH AREA: Circadian clock; Neuroscience -- DISEASE AREA: Neurodegeneration; Cancer