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AdipoGen Life Sciences
Rottlerin
50
CHF
CHF 50.00
In stock
AG-CN2-0526-M01010 mgCHF 50.00
AG-CN2-0526-M05050 mgCHF 180.00
| Product Details | |
|---|---|
| Synonyms | Mallotoxin; NSC94525; NSC56346; Kamalin |
| Product Type | Chemical |
| Properties | |
| Formula |
C30H28O8 |
| MW | 516.5 |
| CAS | 82-08-6 |
| RTECS | AM6913800 |
| Source/Host Chemicals | Isolated from Mallotus philippinensis. |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Orange to brown solid. |
| Solubility | Soluble in DMSO (50mg/ml) or ethanol (1mg/ml). Insoluble in water. |
| Identity | Determined by 1H-NMR and MS. |
| InChi Key | DEZFNHCVIZBHBI-ZHACJKMWSA-N |
| Smiles | CC1(C)C=CC2=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C(O)C(C(/C=C/C4=CC=CC=C4)=O)=C2O1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Anticancer agent that can inhibit cell growth, induce apoptosis, autophagy and cell cycle arrest, inhibit cell invasion and shows anti-angiogenic activity.
- OXPHOS inhibitor. Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5'-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS).
- Useful for immunometabolism research.
- Potent activator of multiple Ca2+-sensitive K+ channels. Naturally occurring hERG channel activator. Antioxidant and ROS scavanger. Might have cardioprotective effects.
- Has been widely used as a selective inhibitor of protein kinase Cδ (PKCδ) (IC50=3-6µM), although there has been controversy in the literature over this claim.
- Inhibits CAM kinase III and a wide range of other kinases and non-kinase proteins in vitro. Most potently inhibits PRAK and MAPKAP-K2.
- Induces autophagy by inhibition of mTORC1 signaling.
- Displays neuroprotective effects.
Product References
- Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994)
- Effects of rottlerin, an inhibitor of calmodulin-dependent protein kinase III, on cellular proliferation, viability, and cell cycle distribution in malignant glioma cells: T.G. Parmer, et al.; Cell Growth Differ. 8, 327 (1997)
- Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000)
- Rottlerin is a mitochondrial uncoupler that decreases cellular ATP levels and indirectly blocks protein kinase Cdelta tyrosine phosphorylation: S.P. Soltoff; J. Biol. Chem. 276, 37986 (2001)
- Rottlerin inhibits insulin-stimulated glucose transport in 3T3-L1 adipocytes by uncoupling mitochondrial oxidative phosphorylation: A.G. Kayali, et al.; Endocrinol. 143, 3884 (2002)
- Kinase inhibitors: Not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003)
- Mitochondrial Ca2+-activated K+ channels in cardiac myocytes: a mechanism of the cardioprotective effect and modulation by protein kinase A: T. Sato, et al.; Circulation 111, 198 (2005)
- Mallotoxin is a novel human ether-a-go-go-related gene (hERG) potassium channel activator: H. Zeng, et al.; JPET 319, 957 (2006)
- Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007)
- Neuroprotective effect of protein kinase C delta inhibitor rottlerin in cell culture and animal models of Parkinson's disease: D. Zhang, et al.; J. Pharmacol. Exp. Ther. 322, 913 (2007)
- Rottlerin induces autophagy and apoptotic cell death through a PKC-delta-independent pathway in HT1080 human fibrosarcoma cells: the protective role of autophagy in apoptosis: K.S. Song, et al.; Autophagy 4, 650 (2008)
- Screen for Chemical Modulators of Autophagy Reveals Novel Therapeutic Inhibitors of mTORC1 Signaling: A.D. Balgi, et al.; PLOS One 4, e7124 (2009)
- Rottlerin exhibits antiangiogenic effects in vitro: G. Valacchi, et al.; Chem. Biol. Drug Des. 77, 460 (2011)
- Rottlerin induces autophagy and apoptosis in prostate cancer stem cells via PI3K/Akt/mTOR signaling pathway: D. Kumar, et al.; Cancer Lett. 343, 179 (2014)
- Rottlerin inhibits cell growth, induces apoptosis and cell cycle arrest, and inhibits cell invasion in human hepatocellular carcinoma: J. Shi, et al.; Mol. Med. Rep. 17, 459 (2018)
- Non-conventional rottlerin anticancer properties: E. Maioli, et al.; Arch. Biochem. Biophys. 645, 50 (2018)
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