Biological Activity
Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC50 = 93 nM). Also suppresses NF-κB activation via inhibition of proteasome chymotrypsin-like activity and IKKαβ. Displays antitumor, anti-inflammatory and antimicrobial activities.
Technical Data
| M. Wt | 464.64 |
| Formula | C30H40O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1258-84-0 |
| PubChem ID | 159516 |
| InChI Key | JFACETXYABVHFD-WXPPGMDDSA-N |
| Smiles | O=C2C(O)=C(C)C1=CC=C([C@](CC[C@]5(C)[C@]([H])4C[C@](C)([C@](OC)=O)CC5)(C)[C@@]4(C)CC3)[C@]3(C)C1=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.62 | 25 | |
| ethanol | 4.65 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 464.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.76 mL | 21.52 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Byun et al (2009) Reactive oxygen species-dependent activation of Bax and Poly(ADP)-ribose) polymerase-1 is requried for mitochondrial cell death induced by triterpenoid Pristimerin in human cervical cancer cells. Mol.Pharmacol. 76 734 PMID: 19574249
Tiedemann et al (2009) Identification of a potent natural triterpenoid inhibitor of proteosome chymotrypsin-like activity and NF-κB with antimyeloma activity in vitro and in vivo. Blood 113 4027 PMID: 19096011
King et al (2009) Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem.Biol. 16 1045 PMID: 19875078
Keywords: Pristimerin, supplier, MAGL, MGL, monoacylglycerol, lipase, inhibitors, lipases, NF-kB, NF-kappaB, NF-κB, inhibits, suppresses, activation, nuclear, factor, kappa, B, transcription, factors, NF-kB/IkB, MAGL, MAGL, Tocris Bioscience
