| S1629 |
Orlistat
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Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. This compound treatment reduces proliferation, induces apoptosis and arrests cell cycle.
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Cell Rep, 2025, 44(7):115901
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Acta Pharmacol Sin, 2025, 10.1038/s41401-025-01477-y
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J Cell Sci, 2024, 137(20)jcs262162
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| S2365 |
Tanshinone IIA
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Tanshinone IIA (Tanshinone B) is the most abundant diterpene quinone in Danshen, Salviae miltiorrhizae Radix, a widely prescribed traditional herbal medicine that is used to treat cardiovascular and inflammatory diseases; this compound is a natural monoacylglycerol lipase inhibitor.
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Phytomedicine, 2024, 128:155431
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J Cancer, 2023, 14(13):2481-2490
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Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12663
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| S7364 |
Atglistatin
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Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, high selectivity over other key metabolic lipases.
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Nat Commun, 2025, 16(1):4432
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Int J Nanomedicine, 2025, 20:9019-9030
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J Cell Mol Med, 2025, 29(14):e70693
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| S4904 |
JZL184
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JZL 184 is the first selective inhibitor of monoacylglycerol lipase (MAGL) with IC50 of 8 nM.
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Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
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Biomed Pharmacother, 2022, 149:112798
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J Cardiovasc Transl Res, 2022, 10.1007/s12265-022-10323-z
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| S9404 |
Pristimerin
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Pristimerin is a naturally occurring triterpenoid that has been shown to suppress the proliferation of various cancer cell lines at the concentration (IC50) range of 0.2-4 μM, including those of breast, glioma, prostate, pancreatic, ovarian, colon. This compound can inhibit monoacylglycerol lipase (MGL) with an IC50 of 93 nM through a reversible mechanism.
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Cell Death Dis, 2020, 14;11(4):232
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| S7457 |
XEN445
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XEN445 is a potent and selective endothelial lipase inhibitor with IC50 of 0.237 μM.
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| S7543 |
JW642
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JW642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
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| S9234 |
Schaftoside
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Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. This compound inhibits the expression of TLR4 and MyD88. It also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
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| S6550 |
URB602
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URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG).
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| E5796 |
CAY10499
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CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC₅₀ values of 144 nM for human recombinant monoacylglycerol lipase (MAGL), 90 nM for hormone-sensitive lipase (HSL), and 14 nM for fatty acid amide hydrolase (FAAH). It also inhibits cell growth in MCF-7, MB-231, COV318, OVCAR-3 cancer cell lines.
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| S8823 |
ABX-1431
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ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.
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| S4930 |
Cetilistat
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Cetilistat (ATL962) is a novel highly lipophilic benzoxazinone that inhibits gastrointestinal and pancreatic lipases. It shows a good safety and tolerability profile in vivo.
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| E1752 |
JNJ-42226314
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JNJ-42226314 is a potent, selective, and reversible noncovalent inhibitor of monoacylglycerol lipase (MAGL). It enhances the expression of endocannabinoid 2-arachidonoylglycerol (2-AG) and exhibits antinociceptive efficacy in models of neuropathic and inflammatory pain.
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| S6609 |
JZL195
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JZL195 is a potent inhibitor of both FAAH and MAGL with IC50s of 2 and 4 nM respectively.
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