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.
IC50&Target
IC50: 80 nM (MAGL)
体外研究
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.
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a Ki 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 [H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC50 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 IC50 of 2.1 μM.
Cell Proliferation Assay
Cell 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 IC50s of 7.9, 21, 25, 57, and 15 μM, respectively.
Was inactive against MRC5 (IC50>100 μM).
体内研究
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.
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.
分子式
C22H24FNO3
分子量
369.43
CAS号
2324160-91-8
运输条件
Room temperature in continental US; may vary elsewhere.