2. Epigenetics
  3. DNA Methyltransferase
  4. RG108

RG108  (Synonyms: N-Phthalyl-L-tryptophan; N-フタリル-L-トリプトファン)

製品番号: HY-13642 純度: 99.93%
COA 取扱説明書 Technical Support

RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 48208-26-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $79 在庫あり
25 mg $165 在庫あり
50 mg $264 在庫あり
100 mg $365 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of RG108:

RG108 関連抗体

Top Publications Citing Use of Products

    RG108 purchased from MedChemExpress. Usage Cited in: Genome Biol. 2025 Jul 11;26(1):202.  [Abstract]

    Detection of methylation levels by immunofluorescence (IF) in cells treated with 5-aza-dC or RG108 (150 μM, 3 h).

    RG108 purchased from MedChemExpress. Usage Cited in: Int J Food Sci Tech. 2024 Jul 18.

    RG108 (10 μM, 12 h) mitigated betaine-induced decrease in Keap1 mRNA levels in L02 cells.

    RG108 purchased from MedChemExpress. Usage Cited in: Proc Biol Sci. 2023 Dec 6;290(2012):20232093.  [Abstract]

    A single topical application of RG108 (2 μL of 0.2 mM diluted in DMSO) on the thorax increased mean survival of B. terrestris workers by 43%.

    RG108 purchased from MedChemExpress. Usage Cited in: Proc Biol Sci. 2023 Dec 6;290(2012):20232093.  [Abstract]

    sirt1 was significantly overexpressed in treatment workers one week after treatment with RG108 （a single topical application on the thorax，2 μL of 0.2 mM diluted in DMSO）.

    RG108 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 16.

    RG108 significantly reduces the overall methylation level of the genome in human SK-Hep-1 cells (Fig E and G).

    DNA Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1][2][3].

    IC50 & Target[1]

    CpG methylase M.SssI

    115 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    >200 μM
    Compound: RG-108
    Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay
    		[PMID: 38823264]
    HeLa IC50
    >200 μM
    Compound: RG-108
    Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
    		[PMID: 38823264]
    K562 IC50
    >200 μM
    Compound: RG-108
    Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay
    		[PMID: 38823264]
    MCF7 GI50
    127.9 μM
    Compound: RG108
    Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by XTT assay
    		[PMID: 25801160]
    Sf9 IC50
    315 μM
    Compound: 11, RG-108
    Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid
    Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid
    		[PMID: 25406944]
    Sf9 IC50
    390 μM
    Compound: 11, RG-108
    Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
    Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
    		[PMID: 25406944]
    SiHa IC50
    >200 μM
    Compound: RG-108
    Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay
    Antiproliferative activity against human SiHa cells incubated for 48 hrs by MTT assay
    		[PMID: 38823264]
    体外実験

    RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. Intriguingly, RG108 causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences[1].
    In another study, the synthesis and in vitro analysis of a biotinylated RG108 conjugate is investigated to evaluate the interactions with DNA methyltransferase enzymes[2].
    In a recent study, it is shown RG108 can significantly reduce the DNA methyltransferases activity in SM derived iPS cells as compared to the native SMs[3].

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

    RG108 関連抗体
    分子量

    334.33

    分子式

    C19H14N2O4
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (299.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9911 mL 14.9553 mL 29.9106 mL
    5 mM 0.5982 mL 2.9911 mL 5.9821 mL
    10 mM 0.2991 mL 1.4955 mL 2.9911 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 1 mg/mL (2.99 mM); Clear solution; Need ultrasonic and warming and heat to 70°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    COA (263 KB) HNMR (262 KB) RP-HPLC (245 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    The substrate DNA for the in vitro methylation assay is a 798 bp fragment (−423/+375 relative to the initiation codon) from the promoter region of the human p16Ink4a gene. The methylation reaction contains 350 to 400 ng substrate DNA and 4 units of M.SssI methylase (0.5 μM) in a final volume of 50 μL. Inhibitors are added to final concentrations of 10, 100, 200, and 500 μM, respectively. Reactions are done at 37°C for 2 hours. After completion, the reaction is inactivated at 65°C for 15 minutes and the DNA is purified using PCR Purification kit. Three hundred nanograms of purified DNA is digested for 3 hours at 60°C with 30 units of BstUI and analyzed on 2% Tris-borate EDTA agarose gels.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.9911 mL 14.9553 mL 29.9106 mL 74.7764 mL
    5 mM 0.5982 mL 2.9911 mL 5.9821 mL 14.9553 mL
    10 mM 0.2991 mL 1.4955 mL 2.9911 mL 7.4776 mL
    15 mM 0.1994 mL 0.9970 mL 1.9940 mL 4.9851 mL
    20 mM 0.1496 mL 0.7478 mL 1.4955 mL 3.7388 mL
    25 mM 0.1196 mL 0.5982 mL 1.1964 mL 2.9911 mL
    30 mM 0.0997 mL 0.4985 mL 0.9970 mL 2.4925 mL
    40 mM 0.0748 mL 0.3739 mL 0.7478 mL 1.8694 mL
    50 mM 0.0598 mL 0.2991 mL 0.5982 mL 1.4955 mL
    60 mM 0.0499 mL 0.2493 mL 0.4985 mL 1.2463 mL
    80 mM 0.0374 mL 0.1869 mL 0.3739 mL 0.9347 mL
    100 mM 0.0299 mL 0.1496 mL 0.2991 mL 0.7478 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    RG108 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    RG10848208-26-0N-Phthalyl-L-tryptophanRG 108RG-108DNA MethyltransferaseDNMTsDNA MTasesInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    RG108
    製品番号:
    HY-13642
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.