1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. MAGL

MAGL

Monoacylglycerol lipase (MGL) is a 33 kDa serine hydrolase that catalyses the hydrolysis of monoacylglycerols to their corresponding fatty acids. The enzyme is found both in the brain and in peripheral tissues such as the kidney, ovary, testis, adrenal gland, adipose tissue and heart. The three-dimensional structure of MGL has been elucidated by X-ray crystallography, and the enzyme has been shown to be a dimeric molecule with amphitropic properties, that is, it can exist both in a soluble form and associated with the membrane lipid bilayers. Mutagenesis studies have demonstrated the importance of the catalytic triad of ser122, asp239 and his269 that the enzyme shares with other enzymes in the α/β hydrolase superfamily. The substrate is recruited via a wide hydrophobic tunnel, where it can then interact with the catalytic triad at the end of the tunnel.

MGL inhibitors have lagged behind, but have a potential advantage over FAAH inhibitors in terms of eCB specificity of action given that the N-acylethanolamines are a class of compounds with multiple biological actions.

MAGL Related Products (14):

Cat. No. Product Name Effect Purity
  • HY-15249
    JZL 184 Inhibitor 98.20%
    JZL 184 is a potent, selective and irreversible monoacylglycerol lipase (MAGL) inhibitor with IC50s of 8 nM and 4 µM for inhibition of MAGL and fatty acid amide hydrolase in mouse brain membranes, respectively.
  • HY-15250
    JZL195 Inhibitor 99.75%
    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.
  • HY-100337
    WWL70 Inhibitor 99.98%
    WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
  • HY-18977
    KML29 Inhibitor 99.21%
    KML29 is a potent and selective MAGL inhibitor with IC50 = 5.9, 15, and 43 nM in human, mouse, and rat brain proteomes, respectively.
  • HY-114157
    DO-264 Inhibitor
    DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
  • HY-114926
    KT185 Inhibitor
    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  • HY-111538
    MAGL-IN-1 Inhibitor
    MAGL-IN-1 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.
  • HY-111512
    PF-06795071 Inhibitor
    PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM.
  • HY-117632
    ABX-1431 Inhibitor 99.96%
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • HY-12332
    JW 642 Inhibitor 99.70%
    JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
  • HY-120215
    KT203 Inhibitor
    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.
  • HY-120177
    KT182 Inhibitor
    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.
  • HY-101457
    JZP-430 Inhibitor >99.0%
    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  • HY-108613
    JJKK 048 Inhibitor
    JJKK 048 is an ultrapotent and highly selective inhibitor of Monoacylglycerol lipase (MAGL).
Isoform Specific Products

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