Rottlerin

製品コードS7862 バッチS786201

印刷

化学情報

Chemical Structure Synonyms Mallotoxin, NSC 56346, NSC 94525 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C30H28O8
分子量 516.54 CAS No. 82-08-6
Solubility (25°C)* 体外 DMSO 11 mg/mL (21.29 mM)
Ethanol 1 mg/mL (1.93 mM)
Water ˂1 mg/mL
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.550mg/ml (1.06mM) Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.550mg/ml (1.06mM) Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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 this compound are detected in cell lysates from rottlerin-treated HPAF-II cells. These data indicate that it 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 this compound is detected in tumor and plasma in mice fed this compound diet. These data indicate that this compound is efficiently absorbed in vivo and suggest a strong potential for this compound as a preventive or adjuvant supplement for pancreatic cancer.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HPAF-II cells
濃度 25 μM
反応時間 3 h, 24 h
実験の流れ

The accumulation of Rottlerin is examined in HPAF-II cells treated with 25 μM of this compound, and the fate of this chemical in the incubation media. Cells are collected at 3 and 24 h after its 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.
動物実験 動物モデル nude mice injected with HPAF-II cells
投薬量 120 mg/kg
投与方法 Oral gavage

参考

  • https://pubmed.ncbi.nlm.nih.gov/8123051/
  • https://pubmed.ncbi.nlm.nih.gov/24482742/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Rottlerin inhibits PKCδ to attenuate pulmonary fibrosis by suppressing NLRC4/ASC-mediated pyroptosis [ Phytomedicine, 2025, 146:157154] PubMed: 40819638
Bryostatin-1 improves function in arteries with suppressed endothelial cell autophagy [ Geroscience, 2025, 10.1007/s11357-025-01650-5] PubMed: 40220153
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。