MAGL-IN-1

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL , with an IC 50 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 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 IC 50 s ranging from 7.9 to 57 μM. MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a K i of 39 nM. MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM. MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [ 3 H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC 50 of 193 nM. 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 IC 50 of 2.1 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: HCT116, MDA-MB-231, CAOV3, OVCAR3, SKOV3, and MRC5 cells Concentration: 0.02-200 μM Incubation Time: 96 hours Result: Inhibited the growth of human breast MDA-MB-231, colorectal HCT116, and ovarian CAOV3, OVCAR3, and SKOV3 cancer cells, with IC 50 s of 7.9, 21, 25, 57, and 15 μM, respectively. Was inactive against MRC5 (IC 50 >100 μM). 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL6 mice, 8-10 weeks old Dosage: 50 mg/kg Administration: Intraperitoneal injection; once Result: Increased 2-AG levels in the brain and plasma. IC50& Target:IC50: 80 nM (MAGL)

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