MAGL
Monoacylglycerol lipase
Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays a crucial role catalysing the hydrolysis of monoglycerides into glycerol and fatty acids. MAGL links the endocannabinoid and eicosanoid systems together by degradation of the abundant endocannabinoid 2-arachidaoylglycerol into arachidonic acid, the precursor of prostaglandins and other inflammatory mediators.
MAGL plays a critical role in lipid signalling: i) it is the major enzyme that controls the levels of 2-AG, an important lipid with various neuroprotective effects; ii) inactivation of MAGL induces an elevation in brain levels of 2-AG and a reduction of AA, a key precursor of pro-inflammatory prostaglandins, resulting in the reduction of neuroinflammation; iii) MAGL regulates the levels of free fatty acids (FFAs) in aggressive cancer cells, and this MAGL-promoted fatty acid network drives a number of pro-tumorigenic signalling pathways. MAGL is emerging as a promising drug target for various diseases.
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MAGL Related Products (85)
- JZL 184
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- CAY10499
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Elcubragistat
0 ImagesSynonyms: ABX-1431 -
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KT109
0 ImagesKT109 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. -
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- ABD957
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AM9928
0 ImagesCat. No.: HY-182639CAS No.: 1869033-49-7AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki 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. -
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- MJN110
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DO-264
0 ImagesDO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM. -
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- JZL195
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- ML-211
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WWL70
0 ImagesWWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM. -
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KML29
0 ImagesKML29 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. -
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JNJ-42226314
0 ImagesJNJ-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. -
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KT182
0 ImagesKT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells. -
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JJH260
0 ImagesJJH260 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. -
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KT203
0 ImagesKT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells. -
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Arachidonoyl Serinol
0 ImagesCat. No.: HY-121476CAS No.: 183718-70-9 -
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JJKK 048
0 ImagesJJKK 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. -
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Euphol
0 ImagesEuphol 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. -
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