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Rottlerin
| Product Name | Rottlerin |
| Price: | Inquiry |
| Catalog No.: | CN06348 |
| CAS No.: | 82-08-6 |
| Molecular Formula: | C30H28O8 |
| Molecular Weight: | 516.5 g/mol |
| Purity: | >=98% |
| Type of Compound: | Miscellaneous |
| Physical Desc.: | Powder |
| Source: | The herbs of Ehretia macrophylla |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(c1c(O)c(Cc2c(O)c(C)c(c(c2O)C(=O)C)O)c(c2c1OC(C)(C)C=C2)O)/C=C/c1ccccc1 C30H28O8 |
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| Description | Rottlerin is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. |
| Target | PKCδ:3 μM (IC50, Porcine spleen) PKCα:30 μM (IC50, baculovirus-infected Sf9 insect cells) PKCγ:40 μM (IC50, baculovirus-infected Sf9 insect cells) PKCβ:42 μM (IC50, baculovirus-infected Sf9 insect cells) PKCη:82 μM (IC50, baculovirus-infected Sf9 insect cells) PKCζ:100 μM (IC50, baculovirus-infected Sf9 insect cells) PKCε:100 μM (IC50, baculovirus-infected Sf9 insect cells) CaM kinase III:5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas) CKII:30 μM (IC50, holoenzyme expressed in E.coli) PKA:78 μM (IC50, catalytic subunit from porcine heart) |
| In Vitro | Rottlerin is a powerful inhibitor of the Ca2+-unresponsive PKCδ with an IC50 of 3 μM for the enzyme from porcine spleen and 6 μM for the recombinant enzyme from baculovirus-infected Sf9 insect cells. Other PKC isoenzymes provestobe at least one order of magnitude less sensitive for Rottlerin. The IC50 values for the different PKC isoenzymes increased in the following order: δ |
| Cell Assay | Cells (5×103/well) are plated in 96-well microtiter plates in 100 μL of growth medium, and after overnight attachment, are exposed for 3 days to a range of concentrations of sorafenib and Rottlerin (0, 0.1, 0.2, 0.4, 0.8, 1.5, 3, 6, 12, 25, 50 μM), alone and in combination. Control cells receive vehicle alone (DMSO). After the treatment, cells are washed, and the number of viable cells is determined using a colorimetric cell proliferation assay. To perform the assay, 20 μL of MTS/phenazine methosulfate solution is added to each well, and after 1 h of incubation at 37°C in a humidified 5% CO2 atmosphere, absorbance is measured at 490 nm in a microplate reader. To directly assess cellular toxicity, 2.5×105 cells are seeded in 60-mm Petri dishes and treated with selected concentrations of inhibitors or vehicle[2]. |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 800.4±65.0 °C at 760 mmHg |
| Flash Point | 266.0±27.8 °C |
| Exact Mass | 516.178406 |
| PSA | 144.52000 |
| LogP | 8.66 |
| Vapour Pressure | 0.0±2.9 mmHg at 25°C |
| Storage condition | 2-8°C |