Rottlerin

Catalog No.S7862 Batch:S786201

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Technical Data

Formula

C30H28O8
Molecular Weight 516.54 CAS No. 82-08-6
Solubility (25°C)* In vitro DMSO 11 mg/mL (21.29 mM)
Ethanol 1 mg/mL (1.93 mM)
Water ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)		 View More
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 Assay:

[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 Study:

[2]
  • Animal Models

    nude mice injected with HPAF-II cells

  • Dosages

    120 mg/kg

  • Administration

    Oral gavage

Selleck's Rottlerin has been cited by 11 publications

Upregulation of rate-limiting enzymes in cholesterol metabolism by PKCδ mediates endothelial apoptosis in diabetic wound healing [ Cell Death Discov, 2024, 10(1):263] PubMed: 38811564
Mitochondrial pyruvate carrier inhibition initiates metabolic crosstalk to stimulate branched chain amino acid catabolism [ Mol Metab, 2023, 70:101694] PubMed: 36801448
Polyaniline-Based Glyco-Condensation on Au Nanoparticles Enhances Immunotherapy in Lung Cancer [ ACS Appl Mater Interfaces, 2022, 14(21):24144-24159] PubMed: 35579575
Revealing the suppressive role of protein kinase C delta and p38 mitogen-activated protein kinase (MAPK)/NF-κB axis associates with lenvatinib-inhibited progression in hepatocellular carcinoma in vitro and in vivo [ Biomed Pharmacother, 2022, 145:112437] PubMed: 34864311
Theaflavin-3,3'-di-gallate represses prostate cancer by activating the PKCδ/aSMase signaling pathway through a 67 kDa laminin receptor [ Food Funct, 2022, 10.1039/d1fo04198c] PubMed: 35302141
Impact of Liver Inflammation on Bile Acid Side Chain Shortening and Amidation [ Cells, 2022, 11(24)3983] PubMed: 36552746
Cooperation of Striatin 3 and MAP4K4 promotes growth and tissue invasion [ Commun Biol, 2022, 5(1):795] PubMed: 35941177
Ubash3b promotes TPA-mediated suppression of leukemogenesis through accelerated downregulation of PKCδ protein [ Biochimie, 2021, 184:8-17] PubMed: 33556471
The MAP4K4-STRIPAK complex promotes growth and tissue invasion in medulloblastoma [ bioRxiv, 2021, 10.1101/2021.05.07.442906] PubMed: None
A strategy for developing effective orally-delivered nanoparticles through modulation of the surface "hydrophilicity/hydrophobicity balance" [ J Mater Chem B, 2017, 5(6):1302-1314] PubMed: 32263598

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.