MAGL Inhibitor

JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC₅₀ of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH.

CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC₅₀ values of 144 nM and 14 nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. Additionally, CAY10499 exhibits anti-inflammatory and antiviral activities.

Elcubragistat (ABX-1431) is a highly effective, selective, orally active, and blood-brain barrier-permeable monoacylglycerol lipase (MAGL) inhibitor, with an IC₅₀ value of 14 nM.

KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC₅₀ of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC₅₀=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-Arachidonoylglycerol (HY-W011051), Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages.

ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, with an IC₅₀ of 0.21 μM for ABHD17B. ABD957 can block N-Ras signaling and the growth of NRAS-mutant AML cells.

AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC₅₀ and K_i values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer.

MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC₅₀s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively. MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity.

DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC₅₀ of 11 nM.

JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC₅₀s of 2 and 4 nM, respectively.

ML-211 is a potent dual inhibitor of LYPLA1 and LYPLA2 enzymes, with an IC₅₀ value of 17 nM against LYPLA1, 30 nM against LYPLA2, and 10 nM against ABHD11.

WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC₅₀ of 70 nM.

KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC₅₀ values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.

JNJ-42226314, a chemical probe, is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.

KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC₅₀ of 0.24 nM in Neuro2A cells.

JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC₅₀ values of 0.50 μM and 0.57 μM, respectively.

KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC₅₀ of 0.31 nM in Neuro2A cells.

Arachidonoyl Serinol, an endogenous cannabimimetic metabolite, is an inhibitor of monoacylglycerol lipase (MAGL). Arachidonoyl Serinol inhibits the hydrolysis of [³H]2-oleoylglycerol and [³H]anandamide with IC₅₀s of ～70 μM.

JJKK 048 is a highly selective and potent monoacylglycerol lipase (MAGL) inhibitor with IC₅₀ values of 214 pM, 275 pM and 363 pM for human, rat, and mouse MAGL. JJKK 048 displays low cross-reactivity with other endocannabinoid targets. JJKK 048 can be used in the research of diseases such as cancer, neurodegenerative diseases, and pain.

Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC₅₀=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.

JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.