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.

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

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.

Y-320 is a new phenylpyrazoleanilide immunomodulator.

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).

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.

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

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.

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.

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.

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).

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

JZL195 is a selective and efficacious dual FAAH MAGL inhibitor.

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.

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.

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

Lipase, triacylglycerol (Alkaline lipase) is a specific enzyme that plays an important role in the catabolism of triacylglycerol to glycerol and fatty acids and is required for the transfer of fatty acids to various tissues of the body, and whose transcriptional receipt of transcripts is subjected to nutrient hormonal regulation and is capable of being upregulated by PPARγ,TNFα downregulation, and insulin-mediated downregulation of FOXO1 nuclear localization.

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

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)

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).