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 |
| Storage | Store at +4°C |
| CAS Number | 82-08-6 |
| PubChem ID | 5281847 |
| InChI Key | DEZFNHCVIZBHBI-ZHACJKMWSA-N |
| Smiles | CC(=O)C1=C(O)C(CC2=C(O)C(C(=O)C=CC3=CC=CC=C3)=C3OC(C)(C)C=CC3=C2O)=C(O)C(C)=C1O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.33 | 20 | |
| ethanol | 1.03 | 2mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 516.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.94 mL | 9.68 mL | 19.36 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Rottlerin, supplier, Reported, PKCdelta, inhibitors, inhibits, Protein, Kinases, C, Protein, Kinase, C, Autophagy, Protein, Kinase, C, Tocris Bioscience
