JW651 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). JW651 inhibited mouse MAGL with an IC50 ~38 nM compared to 10,380 for ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG and >100,000 for FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). JW651 was used as the MAGL inhibitor along with JW912, a fluorescent inihibitor of both MAGL and ABHD6.
JW651 is a potent selective inhibitor of MAGL; active in vivo.
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Cell chemical biology, 27(2), 143-157 (2020-01-25)
Salinipostin A (Sal A) is a potent antiplasmodial marine natural product with an undefined mechanism of action. Using a Sal A-derived activity-based probe, we identify its targets in the Plasmodium falciparum parasite. All of the identified proteins contain α/β serine
The Cravatt group develops innovative technologies to understand enzyme roles in disease, focusing on activity-based protein profiling.
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