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^[1]. IC50 & Target: IC50: 80 nM (MAGL)^[1] In Vitro: MAGL-IN-1 (compound 23) (0.02-200 μM; 96 h) produces an appreciable inhibition of cell viability in all the tested cancer cell lines, with IC₅₀s ranging from 7.9 to 57 μM^[1].
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a K_i of 39 nM^[1].
MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM^[1].
MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [³H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC₅₀ of 193 nM^[1].
MAGL-IN-1 (0.01-30 μM; 15 min) inhibits 2-OG hydrolysis in a concentration-dependent manner in mouse brain membrane preparations, with an IC₅₀ of 2.1 μM^[1]. In Vivo: MAGL (compound 23) (50 mg/kg; a single i.p.) increases the 2-AG level in plasma and brain, and does not alter anandamide (AEA), arachidonic acid and prostaglandin levels in plasma and brain of mice^[1].