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 (86)
Related Products (86)
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ML-226
0 ImagesML226 is a potent inhibitor of α/β hydrolase domain protein 11 (ABHD11), with in vitro and in situ IC50 values of 15 and 0.68 nM, respectively. ML226 is an inhibitor of protein palmitoylthioesterase lysophospholipase 1 (LYPLA1) and LYPLA2. ML226 can be used for research related to neurological diseases.
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MAGL-IN-1
0 ImagesMAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.
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SR-4559
0 ImagesSR-4559 is a α/β hydrolase domain-containing protein 5 (ABHD5) ligand. SR-4559 activates adipose triglyceride lipase (ATGL) and stimulates lipolysis by inhibiting ABHD5-PLIN interactions in adipocytes and muscle cells. SR-4559 can be used for metabolic diseases like Chanarin Dorfman syndrome research.
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ABC34
0 ImagesABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122.
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JZP-MA-11
0 ImagesJZP-MA-11 is a brain-penetrant positron emission tomography (PET) ligand targeting the brain endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP).
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FAAH/MAGL-IN-5
0 ImagesCat. No.: HY-77491CAS No.: 1010096-65-7AM6701 is a potent FAAH/MAGL inhibitor (equipotent inhibitory IC50: 1.2 nM) with neuroprotective effects.
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MAGL-IN-4
0 ImagesMAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.
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JZP-361
0 ImagesJZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.
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LEI-106
0 ImagesLEI-106 is a dual ABHD6 and DAGL-α inhibitor, with a Ki of 0.8 μM for ABHD6, and an IC50 of 18 nM and a Ki of 0.7 μM for DAGL-α. LEI-106 blocks the synthesis of 2-arachidonoylglycerol, reduces the level of endothelial cell-derived 2-arachidonoylglycerol, without altering the levels of cannabinoids and diacylglycerol. LEI-106 is applicable to research related to diet-induced obesity and metabolic syndrome.
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KT185
0 ImagesKT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
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WWL123 analogue-1
0 ImagesWWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
