Triterpenoid. Antitumor agent. Induces caspase-dependent apoptosis by inhibiting the chymotrypsin-like activity of the proteasome. Inhibits NF-κB activation via inhibition of IKKα or IKKβ. Inhibits induction of inducible nitric oxide synthase (iNOS; NOS II). Shows in vitro antimalarial and insecticidal activity. Induces mitochondrial cell death. Has antiproliferative, antifungal and antiviral properties. Potent and reversible monoacylglycerol lipase (MGL) inhibitor.
Product Details
| Alternative Name: | Celastrol methyl ester |
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| Formula: | C30H40O4 |
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| MW: | 464.6 |
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| Source: | Isolated from Tripterygium wilfordii Hook.F. |
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| CAS: | 1258-84-0 |
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| MI: | 14: 10370 |
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| Purity: | ≥97% (HPLC) |
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| Identity: | Determined by IR. |
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| Appearance: | Orange crystalline solid. |
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| Solubility: | Soluble in DMSO or ethyl acetate; insoluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Pristimerin Inhibits Prostate Cancer Bone Metastasis by Targeting PC-3 Stem Cell Characteristics and VEGF-Induced Vasculogenesis of BM-EPCs: S. Huang, et al.; Cell. Physiol. Biochem.
37, 253 (2015),
Application(s): Cell culture,
Abstract;
Full Text
Discovery of potent and reversible monoacylglycerol lipase inhibitors: A.R. King, et al.; Chem. Biol.
16, 1045 (2009),
Abstract;
Identification of a potent natural triterpenoid inhibitor of proteosome chymotrypsin-like activity and NF-kappaB with antimyeloma activity in vitro and in vivo: R.E. Tiedemann, et al.; Blood
113, 4027 (2009),
Abstract;
Reactive oxygen species-dependent activation of Bax and poly(ADP-ribose) polymerase-1 is required for mitochondrial cell death induced by triterpenoid pristimerin in human cervical cancer cells: J.Y. Byun, et al.; Mol. Pharmacol.
76, 734 (2009),
Abstract;
Triterpenoids as new promising anticancer drugs: A. Petronelli, et al.; Anticancer Drugs
20, 880 (2009),
Abstract;
Antiproliferative activity of pristimerin isolated from Maytenus ilicifolia (Celastraceae) in human HL-60 cells: P.M. Costa, et al.; Toxicol. in vitro
22, 854 (2008),
Abstract;
Pristimerin induces apoptosis by targeting the proteasome in prostate cancer cells: H. Yang, et al.; J. Cell. Biochem.
103, 234 (2008),
Abstract;
Anticytomegalovirus activity of pristimerin, a triterpenoid quinone methide isolated from Maytenus heterophylla (Eckl. & Zeyh.): T. Murayama, et al.; Antivir. Chem. Chemother.
18, 133 (2007),
Abstract;
Antigiardial activity of triterpenoids from root bark of Hippocratea excelsa: G.J. Mena-Rejón, et al.; J. Nat. Prod.
70, 863 (2007),
Abstract;
Antifungal properties of pristimerin and celastrol isolated from Celastrus hypoleucus: D.Q. Luo, et al.; Pest Manag. Sci.
61, 85 (2005),
Abstract;
Pristimerin induces caspase-dependent apoptosis in MDA-MB-231 cells via direct effects on mitochondria: C.C. Wu, et al.; Mol. Cancer Ther.
4, 1277 (2005),
Abstract;
Full Text
Antitumor agents. 228. five new agarofurans, Reissantins A-E, and cytotoxic principles from Reissantia buchananii: F.R. Chang, et al.; J. Nat. Prod.
66, 1416 (2003),
Abstract;
Release of intermediate reactive hydrogen peroxide by macrophage cells activated by natural products: R.R. Moreira, et al.; Biol. Pharm. Bull.
24, 201 (2001),
Abstract;
Full Text
Insecticidal activity of Maytenus species (Celastraceae) nortriterpene quinone methides against codling moth, Cydia pomonella (L.) (Lepidoptera: tortricidae): J. Avilla, et al.; J. Agric. Food Chem.
48, 88 (2000),
Abstract;
Novel quinone methides from Salacia kraussii with in vitro antimalarial activity: J.N. Figueiredo, et al.; J. Nat. Prod.
61, 718 (1998),
Abstract;
The triterpenoid quinonemethide pristimerin inhibits induction of inducible nitric oxide synthase in murine macrophages: V.M. Dirsch, et al.; Eur. J. Pharmacol.
336, 211 (1997),
Abstract;
Structure of pristimerin: A.B. Kulkarni & R.C. Shah; Nature
173, 1237 (1954),
Abstract;
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