KT182 is a very potent, orally bioavailable, selective inhibitor of ABHD6 (a/b-Hydrolase Domain Containing 6). IC50 = 1.7 nM. KT182 inhibits ABHD6 activity in the brain and liverin mice (ip administration).
Journal of medicinal chemistry, 56(21), 8270-8279 (2013-10-25)
α/β-Hydrolase domain containing 6 (ABHD6) is a transmembrane serine hydrolase that hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to regulate certain forms of cannabinoid receptor-dependent signaling in the nervous system. The full spectrum of ABHD6 metabolic activities and functions is currently
The Cravatt group develops innovative technologies to understand enzyme roles in disease, focusing on activity-based protein profiling.
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