Rottlerin
Chemical Name: 3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophenone
Purity: ≥95%
Biological Activity
Originally reported to inhibit PKC isoforms. Also reported to inhibit CAM kinase III. However, recently shown to inhibit a wide range of protein kinases, and most potently to inhibit PRAK and MAPKAP-K2 (IC50 values are 1.9 and 5 μM respectively). Also shown to act as a direct mitochondrial uncoupler. Thought to stimulate autophagy by targeting upstream mTORC1 control pathways.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Specificity and mechanism of action of some commonly used protein kinase inhibitors.
Davies et al.
Biochem.J., 2000;351:95 -
Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling.
Balgi et al.
PLoS One, 2009;4:e7124 -
Rottlerin, a novel protein kinase inhibitor.
Gschwendt et al.
Biochem.Biophys.Res.Commun., 1994;199:93 -
Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson's disease.
Zhang et al.
J.Pharmacol.Exp.Ther., 2007;322:913
Product Datasheets
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Citations for Rottlerin
The citations listed below are publications that use Tocris products. Selected citations for Rottlerin include:
6 Citations: Showing 1 - 6
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Chronic interleukin-1 exposure drives haematopoietic stem cells towards precocious myeloid differentiation at the expense of self-renewal.
Authors: Pietras Et al.
Nat Cell Biol 2016;18:607
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Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals.
Authors: Shu Et al.
PLoS One 2014;9:e95259
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Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes.
Authors: Seto Et al.
Bladder (San Franc) 2013;8:e66404
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Treatment of experimental asthma using a single small molecule with anti-inflammatory and BK channel-activating properties.
Authors: Goldklang Et al.
FASEB J 2013;27:4975
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High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival.
Authors: Barbaric Et al.
J Biomol Screen 2011;16:603
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A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors.
Authors: Schaertl Et al.
J Biomol Screen 2010;15:478
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