pristimerin
Synonym(s):(9b,13a,14b,20a)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26 -trinoroleana-1(10),3,5,7-tertraen-29-oic acid methyl ester;Celastrol methyl ester;Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II;Pristimerin - CAS 1258-84-0 - Calbiochem
- CAS NO.:1258-84-0
- Empirical Formula: C30H40O4
- Molecular Weight: 464.64
- MDL number: MFCD01711331
- EINECS: 251-228-4
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-09-15 15:02:29
What is pristimerin?
Description
Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-
The Uses of pristimerin
Pristimerin is a triterpenoid that inhibits tumor angiogenesis by targeting VEGFR2 activation and is known to exhibit anti-inflammatory properties.
The Uses of pristimerin
antineoplastic, antiinflammatory
What are the applications of Application
Pristimerin is a triterpenoid and inducer of caspase-dependent apoptosis
Definition
ChEBI: Pristimerin is a carboxylic ester.
General Description
A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii, whose inhibitory activities against proteasome chymotrypsin subunit (IC50 = 2.2 and 3.0 μM against purified rabbit 20S and human 26S proteasome, respectively) and cellular NF-κB pathway/IKK activation most likely account for its reported anticancer efficacy both in vitro (IC50 ≤610 nM in A549, K562, KBM5, MCF-7, MDA-MB-231, HepG2, and primary human leukemia cell cultures) and in mice in vivo (1 to 2.5 mg/kg/day, s.c.), including imatinib/STI571-resistant cancer cells harboring Bcr-Abl T315I mutation. Also reported to inhibit the activity of monoacylglycerol lipase (MGL), the enzyme that hydrolyzes and deactivates the cannabionoid receptor ligand 2-Arachidonoyl-sn-glycerol (2-AG), in a reversible manner with high potency (IC50 = 93 nM).
Biological Activity
Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC 50 = 93 nM). Also suppresses NF- κ B activation via inhibition of proteasome chymotrypsin-like activity and IKK α / β . Displays antitumor, anti-inflammatory and antimicrobial activities.
Properties of pristimerin
Melting point: | 219.5°C |
Boiling point: | 488.1°C (rough estimate) |
Density | 1.0271 (rough estimate) |
refractive index | 1.4800 (estimate) |
storage temp. | -20°C |
solubility | DMSO: ≥5mg/mL |
pka | 8.60±0.70(Predicted) |
form | Red solid |
color | orange |
Safety information for pristimerin
Computed Descriptors for pristimerin
New Products
Tubulysin F Tubulysin D Tubulysin I Tubulysin C Diethyl Aluminium Cyanide (1.0 M in Toluene) Potassium HMDS (1.0 M in THF) Methyl (R)-1-Boc-4,4-difluoropyrrolidine-2-carboxylate CYCLOBUTYLAMINE HYDROCHLORIDE 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) 4,4-DIFLUOROPIPERIDINE 2,2-Difluoropropanol 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Fuel shell Imeglimin Hydrochloride IH Magnesium Trisilicate Lubiprostone Latanoprostene Bunod Flame Retardant Zinc Borate methyl 3-fluoro-4- thiomorpholino phenylcarbamate (R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonateRelated products of tetrahydrofuran
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