1. Epigenetics
    TGF-beta/Smad
  2. PKC

Rottlerin (Synonyms: Mallotoxin; NSC 56346; NSC 94525)

Cat. No.: HY-18980
Handling Instructions

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.

For research use only. We do not sell to patients.

Rottlerin Chemical Structure

Rottlerin Chemical Structure

CAS No. : 82-08-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

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<α, β, γ<η, ζ, ε[1]. Rottlerin inhibits cell proliferation in a dose-dependent manner. The combination of both inhibitors (Sorafenib and Rottlerin) is substantially more effective than either single agent and produces a significant decrease in glioma cell survival. The cytotoxic effect of Rottlerin and Sorafenib is further confirmed using a clonogenic assay. There is a dose-dependent decrease in colony forming ability due to Rottlerin and Sorafenib, when administered independently, with the latter having activity at concentrations above 5 μM. In addition, there is striking potentiation of efficacy when the two agents are administered in combination[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9360 mL 9.6798 mL 19.3596 mL
5 mM 0.3872 mL 1.9360 mL 3.8719 mL
10 mM 0.1936 mL 0.9680 mL 1.9360 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

516.54

Formula

C₃₀H₂₈O₈

CAS No.

82-08-6

SMILES

O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Rottlerin
Cat. No.:
HY-18980
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Rottlerin

Cat. No.: HY-18980