Esterases (Carboxyl)
Phospholipases and acetylcholinesterases are members of the subclass of esterases. Hydrolyzing phospholipids into a carboxylic acid and a lysophospholipid, the PLA1 and PLA2 (EC 3.1.1.4) esterases differentiate from PLC and PLD which are responsible for cleaving either sites of the phophonate bonds present in phospholipids. Due to the importance of PLA2 in inflammatory responses, regulation of the enzyme is essential. PLA2 is regulated by phosphorylation and calcium concentrations. PLA2 is phosphorylated by a MAPK at Serine-505. When phosphorylation is coupled with an influx of calcium ions, PLA2 becomes stimulated and can translocate to the membrane to begin catalysis.[1]
[1] Properties and Regulation of Cytosolic Phospholipase A2. C.C. Leslie. J. Biol. Chem. 1997, 272, 16709-16712.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3000 | ABX-1431 | Highly potent, selective, brain-penetrant, and orally available MAGL inhibitor | €135.00 | |
| 3682 | AMZ30 | Potent, selective and covalent PME-1 inhibitor | €130.00 | |
| 2578 | ASB14780 | Potent, orally available inhibitor of cPLA2α; antiinflammatory drug | €130.00 | |
| 2276 | Atglistatin | Potent and selective inhibitor of adipose triglyceride lipase (ATGL) | €90.00 | |
| 2661 | AZD2716 | Potent secreted phospholipase A2 (sPLA2) inhibitor | €145.00 | |
| 3297 | BChE inhibitor 8012-9656 | Highly potent, selective and brain-penetrant BChE inhibitor | €140.00 | |
| 1609 | CDIBA | cPLA2 inhibitor | €125.00 | |
| 3478 | Dehydroevodiamine hydrochloride | Potent acetylcholinesterase inhibitor | €70.00 | |
| 2982 | DO264 | Potent, selective, and in vivo active ABHD12 inhibitor | €125.00 | |
| 1438 | Donepezil hydrochloride | Acetylcholinesterase inhibitor | €60.00 | |
| 3707 | GLN-1062 | Brain-pentrant prodrug of galantamine; Acetylcholinesterase inhibitor | €120.00 | |
| 3213 | GSK264220A | Potent endothelial lipase (EL) and lipoprotein lipase (LPL) inhibitor | €90.00 | |
| 2486 | JZP 361 | Selective reversible inhibitor of MAGL with Histamine H1 antagonistic activity | €125.00 | |
| 2797 | Lalistat 2 | Selective inhibitor of lysosomal acid lipase (LAL) | €105.00 | |
| 3296 | LEI-301 | Potent phospholipase A and acyltransferase (PLAAT) inhibitor | €140.00 | |
| 2580 | MJN110 | Potent, selective, and in-vivo-active MAGL inhibitor | €85.00 | |
| 3658 | Neostigmine methyl sulfate | Reversible acetylcholinesterase inhibitor | €40.00 | |
| 3500 | Orlistat | Potent, specific and irreversible inhibitor of pancreatic and gastric lipases | €120.00 | |
| 3167 | Rivastigmine tartrate | Centrally selective acetylcholinesterase inhibitor | €60.00 | |
| 2696 | URB602 | Non-competitive inhibitor of MAGL | €60.00 | |
| 4077 | Varespladib | sPLA2 inhibitor | Inquire | |
| 4032 | Varespladib methyl | Secretory phospholipase A2 (sPLA2) inhibitor | Inquire | |