Lipase

Atglistatin is a highly effective, specific and competitive ATGL inhibitor with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, and no toxicity when the concentration up to 50 μM.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

Beta-Sitosterol (SKF 14463) has recently been shown to induce G2 M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K Akt signaling pathways. Beta-Sitosterol (SKF 14463) , a main dietary phytosterol found in plants, may have the potential for prevention and therapy for human cancer. Although the exact mechanism of action of Beta-Sitosterol (SKF 14463) is unknown, it may be related to cholesterol metabolism or anti-inflammatory effects (via interference with prostaglandin metabolism). Beta-Sitosterol (SKF 14463) induces apoptosis and activates key caspases in MDA-MB-231 human breast cancer cells.

MJN110 (Cravatt Reagent) is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110(Cravatt Reagent) Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

JJKK 048 is a potent and selective MAGL inhibitor.

Endothelial lipase inhibitor-1 is a potent inhibitor of endothelial lipase with an IC50 of 49 nM.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological properties and is considered to have anti-inflammatory action.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

WWL70 is a selective inhibitor of alpha beta hydrolase domain 6 with an IC50 of 70 nM.

Lalistat 2 is a selective inhibitor of lysosomal acid lipase with IC50 of 152 nM and exhibits no inhibition of human pancreatic lipase or bovine milk lipoprotein lipase (up to 10 μM).

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

NF-1819 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. NF-1819 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. NF-1819 displays high membrane permeability and brain penetrant.

JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic pain and inflammatory pain.

JZL195 is a selective and efficacious dual FAAH MAGL inhibitor.

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)

ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL MGLL) inhibitor (IC50: 14 nM).

NG-497 is a selective, small molecule inhibitor of human adipose triglyceride lipase (ATGL) that targets the enzymatically active patatin-like structural domain of human ATGL.NG-497 binds ATGL in a hydrophobic lumen adjacent to the active site.NG-497 abrogates lipolysis in human adipocytes in a dose-dependent and reversible manner.NG-497 has been shown to be useful in cancer research. can be used in cancer research.

JZP-430 is an effective, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties.

JZP-361 is a specific MAGL inhibitor with IC50s of 46 nM, 7.24 μM, and 1.79 μM for human recombinant MAGL, human recombinant FAAH, and human hABHD6. JZP-361 displays anti-histaminergic activities. JZP-361 can be used in studies about asthma.

URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.

MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.

PF-06795071 is an effective and selective covalent inhibitor of MAGL (IC50: 3 nM).