Rottlerin

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Cat.No. 1610 - Rottlerin | C30H28O8 | CAS No. 82-08-6
Description: Reported PKCδ inhibitor
Chemical Name: 3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophenone
Datasheet
Citations (3)
Reviews
Literature

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=C\C3=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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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

3 Citations for Rottlerin

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

Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409

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


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Literature in this Area

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