Rottlerin

Catalog No.S7862 Synonyms: Mallotoxin, NSC 56346, NSC 94525

For research use only.

Rottlerin (Mallotoxin, NSC 56346, NSC 94525), a natural compound purified from Mallotus Philippinensis, is a specific Protein kinase inhibitor with IC50 of 3 μM, 6 μM and 5.3 μM for PKCδ(from baculovirus-infected Sf9 insect cells), PKCδ(from porcine spleen) and CaM kinase III, respectively. Rottlerin also inhibits PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM, respectively.

Rottlerin Chemical Structure

CAS No. 82-08-6

Selleck's Rottlerin has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description Rottlerin (Mallotoxin, NSC 56346, NSC 94525), a natural compound purified from Mallotus Philippinensis, is a specific Protein kinase inhibitor with IC50 of 3 μM, 6 μM and 5.3 μM for PKCδ(from baculovirus-infected Sf9 insect cells), PKCδ(from porcine spleen) and CaM kinase III, respectively. Rottlerin also inhibits PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM, respectively.
Targets
PKCδ [1]
(Cell-free assay)
CKIII [1]
(Cell-free assay)
PKCα [1]
(Cell-free assay)
CKII [1]
(Cell-free assay)
PKCγ [1]
(Cell-free assay)
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3 μM 5.3 μM 30 μM 30 μM 40 μM
In vitro

Rottlerin is extracted from the plasma and tissues using protein precipitation-extraction and analyzed by reverse-phase HPLC-DAD method. Significant levels of rottlerin are detected in cell lysates from rottlerin-treated HPAF-II cells. These data indicate that rottlerin is efficiently absorbed in cells in vitro.[2]

In vivo

A xenograft model of pancreatic cancer is prepared by injection of 2×106 HPAF-II cells subcutaneously into nude mice. A substantial amount of Rottlerin is detected in tumor and plasma in mice fed Rottlerin diet. These data indicate that Rottlerin is efficiently absorbed in vivo and suggest a strong potential for Rottlerin as a preventive or adjuvant supplement for pancreatic cancer.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: HPAF-II cells
  • Concentrations: 25 μM
  • Incubation Time: 3 h, 24 h
  • Method:

    The accumulation of Rottlerin is examined in HPAF-II cells treated with 25 μM Rottlerin, and the fate of Rottlerin in the incubation media. Cells are collected at 3 and 24 h after Rottlerin stimulation and conditioned media are taken at 0.5, 1.0, 3.0, 6.0 and 24 h (n=4 for each time point). Samples are prepared immediately for HPLC analysis without further storage.

Animal Research:

[2]

  • Animal Models: nude mice injected with HPAF-II cells
  • Dosages: 120 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 516.54
Formula

C30H28O8

CAS No. 82-08-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=C(C(=C1O)C(=O)C)O)CC2=C(C(=C3C(=C2O)C=CC(O3)(C)C)C(=O)C=CC4=CC=CC=C4)O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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