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Biological Activity for Rottlerin
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 for Rottlerin
|Storage||Store at +4°C|
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.
Solubility Data for Rottlerin
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Rottlerin
The following data is based on the product molecular weight 516.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||9.68 mL||48.4 mL||96.8 mL|
|1 mM||1.94 mL||9.68 mL||19.36 mL|
|2 mM||0.97 mL||4.84 mL||9.68 mL|
|10 mM||0.19 mL||0.97 mL||1.94 mL|
References for Rottlerin
References are publications that support the biological activity of the product.
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Gschwendt et al (1994) Rottlerin, a novel protein kinase inhibitor. Biochem.Biophys.Res.Commun. 199 93 PMID: 8123051
Zhang et al (2007) Neuroprotective effect of protein kinase Cδ inhibitor rottlerin in cell culture and animal models of Parkinson's disease. J.Pharmacol.Exp.Ther. 322 913 PMID: 17565007
Balgi et al (2009) Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4 e7124 PMID: 19771169
If you know of a relevant reference for Rottlerin, please let us know.
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Keywords: Rottlerin, Rottlerin supplier, Reported, PKCdelta, inhibitors, inhibits, Protein, Kinases, C, Kinase, Autophagy, 1610, Tocris Bioscience
6 Citations for Rottlerin
Citations are publications that use Tocris products. Selected citations for Rottlerin include:
Pietras et al (2016) Chronic interleukin-1 exposure drives haematopoietic stem cells towards precocious myeloid differentiation at the expense of self-renewal. Nat Cell Biol 18 607 PMID: 27111842
Barbaric et al (2011) High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival. J Biomol Screen 16 603 PMID: 21593487
Seto et al (2013) Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes. Bladder (San Franc) 8 e66404 PMID: 23799098
Shu et al (2014) Orexin-A promotes cell migration in cultured rat astrocytes via Ca2+-dependent PKCα and ERK1/2 signals. PLoS One 9 e95259 PMID: 24748172
Goldklang et al (2013) Treatment of experimental asthma using a single small molecule with anti-inflammatory and BK channel-activating properties. FASEB J 27 4975 PMID: 23995289
Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409
Do you know of a great paper that uses Rottlerin from Tocris? Please let us know.
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Literature in this Area
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