AKU-005|CAS 1515855-85-2|DC Chemicals

Cas No.:	1515855-85-2
Chemical Name:	AKU-005
SMILES:	O=C(N1CCN(C(C2=CC=CC=C2)C3=CC=CC=C3)CC1)N4N=CN=C4
Formula:	C₂₀H₂₁N₅O
M.Wt:	347.42

Cat. No.	Product name	Field of application
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.
DC44076	MAGL-IN-1	MAGL-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.
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.