| DC46532 |
MAGL-IN-4
|
MAGL-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. |
| DC73754 |
AKU-005
|
AKU-005 is a potent, dual MAGL/FAAH inhibitor with IC50 of 589 and 309 pM for MAGL in rat and mouse brain membrane respectively, inhibits rat and human FAAH with IC50 of 63 and 389 nM. |
| DC71679 |
JZP-361
|
JZP-361 is a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50=1.79 μM). JZP-361 represents a dual-acting pharmacological tool possessing both MAGL inhibitory and antihistaminergic activities. |
| DC70189 |
AM9928
|
AM9928 is a potent, covalent monoacylglycerol lipase (MAGL) inhibitor with IC50 of 8.9 nM (hMAGL).AM9928 covalently binds to and inactivates MAGL by carbamylation of the enzyme's catalytic Ser122 nucleophile.AM9928 inhibited adhesion and transmigration of breast cancer cells through human brain microvascular endothelial cells (HBMECs), inhibited TNBC's secretion of inflammatory cytokines such as IL-6 and IL-8, and the angiogenic factor VEGF-A.AM9928 inhibited in vivo changes in BBB permeability and decreased TNBC colonization in brain.MAGL inhibitor AM9928 is a novel treatment of TNBC tumor growth and TNBC-colonization in the brain. |
| DC70188 |
AM6580
|
AM6580 is a potent, covalent monoacylglycerol lipase (MAGL) inhibitor with IC50 of 3 nM (hMAGL).AM6580 covalently binds to and inactivates MAGL by carbamylation of the enzyme's catalytic Ser122 nucleophile. |
| DC50249 |
Monoacylglycerol lipase inhibitor 1
|
Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13). |
| DC50248 |
LEI-106
|
LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM. |
