Rottlerin

CHF 50.00
In stock
AG-CN2-0526-M01010 mgCHF 50.00
AG-CN2-0526-M05050 mgCHF 180.00
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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
  • 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
  1. Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994)
  2. 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)
  3. Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000)
  4. 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)
  5. Rottlerin inhibits insulin-stimulated glucose transport in 3T3-L1 adipocytes by uncoupling mitochondrial oxidative phosphorylation: A.G. Kayali, et al.; Endocrinol. 143, 3884 (2002)
  6. Kinase inhibitors: Not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003)
  7. 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)
  8. Mallotoxin is a novel human ether-a-go-go-related gene (hERG) potassium channel activator: H. Zeng, et al.; JPET 319, 957 (2006)
  9. Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007)
  10. 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)
  11. 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)
  12. Screen for Chemical Modulators of Autophagy Reveals Novel Therapeutic Inhibitors of mTORC1 Signaling: A.D. Balgi, et al.; PLOS One 4, e7124 (2009)
  13. Rottlerin exhibits antiangiogenic effects in vitro: G. Valacchi, et al.; Chem. Biol. Drug Des. 77, 460 (2011)
  14. 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)
  15. 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)
  16. Non-conventional rottlerin anticancer properties: E. Maioli, et al.; Arch. Biochem. Biophys. 645, 50 (2018)
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