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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
Purity: ≥95% (HPLC)
Citations (6)

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

M. Wt 516.55
Formula C30H28O8
Storage Store at +4°C
Purity ≥95% (HPLC)
CAS Number 82-08-6
PubChem ID 5281847
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Rottlerin

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 10.33 20

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Rottlerin

Certificate of Analysis / Product Datasheet
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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

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

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

Seto et al (2013) Acute SimV. 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

Do you know of a great paper that uses Rottlerin from Tocris? Please let us know.

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