Home TGF-beta/Smad PKC inhibitor Rottlerin For research use only.

Rottlerin

Synonyms: Mallotoxin, NSC 56346, NSC 94525

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

Rottlerin Chemical Structure

CAS: 82-08-6

Selleck's Rottlerin has been cited by 10 publications

Purity & Quality Control

Batch: S786201 DMSO] 11 mg/mL] false] Ethanol] 1 mg/mL] false] Water] ˂1 mg/mL] false Purity: 98.06%
98.06

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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)		 Click to View More Targets
3 μM 5.3 μM 30 μM 30 μM 40 μM
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models nude mice injected with HPAF-II cells
Dosages 120 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 516.54 Formula

C30H28O8
CAS No. 82-08-6 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 11 mg/mL ( (21.29 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : ˂1 mg/mL


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In vivo
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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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