Rottlerin

Cat. No. 1610

Rottlerin C30H28O8 [82-08-6]

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Chemical Name: 3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophenone

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

M.Wt:
516.55
Formula:
C30H28O8
Solubility:
Soluble to 2 mM in ethanol with gentle warming and to 20 mM in DMSO
Storage:
Store at +4°C
CAS No:
82-08-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Balgi et al (2009) Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4 e7124. PMID: 19771169.

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.

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.

If you know of a relevant reference for Rottlerin please let us know.

Citations are publications that use Tocris products. Selected citations for Rottlerin include:

Seto et al (2013) Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes. Bladder (San Franc) 8 e66404. PMID: 23799098.

Barbaric et al (2011) High-content screening for chemical modulators of embryonal carcinoma cell differentiation and survival. J Biomol Screen 16 603. PMID: 21593487.

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? If so please let us know.

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Keywords: Rottlerin, supplier, Reported, PKCdelta, inhibitors, inhibits, Protein, Kinases, C, Tocris Bioscience, Protein Kinase C Inhibitor products

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