2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. ART558

ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer.

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CAS 番号 : 2603528-97-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 在庫あり
Solution
10 mM * 1 mL in DMSO USD 495 在庫あり
Solid
1 mg $180 在庫あり
5 mg $450 在庫あり
10 mg $760 在庫あり
25 mg $1200 在庫あり
50 mg $1575 在庫あり
100 mg $2120 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

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カスタマーレビュー

Based on 49 publication(s) in Google Scholar

Other Forms of ART558:

ART558 関連抗体

Top Publications Citing Use of Products

顧客検証

Flow Cytometry
Bio/Physico-chemical Assay
WB
Cell Proliferation/Viability Assay

    ART558 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 7.  [Abstract]

    Quantification of the percentage of Annexin V/PI-positive cells assessed by flow cytometry in EP300Mut, EP300WT NA-ATLL cells +/− POLQi (20 μM ART558 for 72 h) and +/− PARPi (10 μM Olaparib for 72 h) was performed.

    ART558 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 3;16(1):9571.  [Abstract]

    ART558 (3 μM; 24 h). Summary comparison between CLEAR-time dPCR (top) and ICE (bottom) 1, 3, and 14 days post-editing.

    ART558 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 6;15(1):9582.  [Abstract]

    HCT116 M-phase deletion SV frequency with POLQ KO and inhibition by ART558 (5–10 µM; 5 h) and novobiocin (NVB) was measured.

    ART558 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 13;14(1):1390.  [Abstract]

    ART558 (ART; 1 μM; 48 h)-mediated inhibition of POLθ leds to activation of the STING pathway in both MDA-MB-436 (left) and CAPAN-1 (right) cells.

    ART558 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2023 Jun 1;133(11):e165934.  [Abstract]

    ART558 (0-2 μM; 6 days) effectively decreases cell viability and inhibits colony formation in colorectal adenocarcinoma cells (DLD-1) with a truncating mutation in BRCA2.

    DNA/RNA Synthesis 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
    RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

    • 生物活性

    • 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

    ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer[1].

    IC50 & Target

    DNA Polymerase

     

    Cellular Effect
    Cell Line Type Value Description References
    DLD-1 EC50
    0.8 1
    Compound: 22; ART558
    Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
    Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
    		[PMID: 36200480]
    DLD-1 EC50
    0.8 1
    Compound: 22; ART558
    Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
    Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
    		[PMID: 36200480]
    DLD-1 EC50
    >12 3
    Compound: 22; ART558
    Antiproliferative activity against human DLD-1 cells
    Antiproliferative activity against human DLD-1 cells
    		[PMID: 36200480]
    DLD-1 EC50
    > 12 3
    Compound: 22; ART558
    Antiproliferative activity against human DLD-1 cells
    Antiproliferative activity against human DLD-1 cells
    		[PMID: 36200480]
    HEK293 EC50
    180 1
    Compound: 22; ART558
    Inhibition of microhomology-mediated end joining in HEK293 cells
    Inhibition of microhomology-mediated end joining in HEK293 cells
    		[PMID: 36200480]
    HEK293 EC50
    180 1
    Compound: 22; ART558
    Inhibition of microhomology-mediated end joining in HEK293 cells
    Inhibition of microhomology-mediated end joining in HEK293 cells
    		[PMID: 36200480]
    体外実験

    ART558 (0-10 μM; 7 days; BRCA2wild-type or BRCA2-/- cells) shows synthetic lethality and a combinatorial effect with the PARPi olaparib in previously described isogenic models of BRCA1-deficiency[1].
    ART558 (5 μM; 0-72 hours; BRCA2wild-type or BRCA2-/- cells) shows γH2AX accumulation in cells[1].
    ART558 inhibits the major Polθ mediated DNA repair process, Theta-Mediated End Joining, without targeting NonHomologous End Joining. ART558 elicits DNA damage and synthetic lethality in BRCA1- or BRCA2-mutant tumour cells and enhances the effects of a PARP inhibitor[1].
    ART558 increases biomarkers of single-stranded DNA and synthetic lethality in 53BP1-defective cells whilst the inhibition of DNA nucleases that promote end-resection reversed these effects, implicating these in the synthetic lethal mechanism-of-action. ART558 increases the residence time of YFP-tagged full-length Polθ at sites of laserinduced DNA damage[1].

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

    ART558 関連抗体

    Cell Viability Assay[1]

    Cell Line: BRCA2wild-type or BRCA2‒/‒ cells
    Concentration: 0~10 μM
    Incubation Time: 7 days
    Result: Showed synthetic lethality and a combinatorial effect with the PARPi olaparib in previously described isogenic models of BRCA1-deficiency.

    Western Blot Analysis[1]

    Cell Line: BRCA2wild-type or BRCA2‒/‒ cells
    Concentration: 5μM
    Incubation Time: 0~72 hours
    Result: Showed γH2AX accumulation in cells.
    分子量

    418.41

    分子式

    C21H21F3N4O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN(C1=CC(C)=CC=C1)C([C@H]2N(C3=C(C(C(F)(F)F)=CC(C)=N3)C#N)CC[C@H]2O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
    溶剤 & 溶解度
    体外: 

    DMSO : 170 mg/mL (406.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3900 mL 11.9500 mL 23.9000 mL
    5 mM 0.4780 mL 2.3900 mL 4.7800 mL
    10 mM 0.2390 mL 1.1950 mL 2.3900 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 (sealed storage, away from moisture and light). 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
    =
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    ×
    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）

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    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    90% Corn Oil

      Solubility: ≥ 5 mg/mL (11.95 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: 4.25 mg/mL (10.16 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 4.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    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: 99.97%

    COA (253 KB) HNMR (229 KB) RP-HPLC (189 KB) LCMS (96 KB)

    取扱説明書 (2659 KB)
    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 (sealed storage, away from moisture and light). 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 2.3900 mL 11.9500 mL 23.9000 mL 59.7500 mL
    5 mM 0.4780 mL 2.3900 mL 4.7800 mL 11.9500 mL
    10 mM 0.2390 mL 1.1950 mL 2.3900 mL 5.9750 mL
    15 mM 0.1593 mL 0.7967 mL 1.5933 mL 3.9833 mL
    20 mM 0.1195 mL 0.5975 mL 1.1950 mL 2.9875 mL
    25 mM 0.0956 mL 0.4780 mL 0.9560 mL 2.3900 mL
    30 mM 0.0797 mL 0.3983 mL 0.7967 mL 1.9917 mL
    40 mM 0.0598 mL 0.2988 mL 0.5975 mL 1.4938 mL
    50 mM 0.0478 mL 0.2390 mL 0.4780 mL 1.1950 mL
    60 mM 0.0398 mL 0.1992 mL 0.3983 mL 0.9958 mL
    80 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7469 mL
    100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5975 mL
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    ART558 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    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:

    ART5582603528-97-6ART 558ART-558DNA/RNA SynthesisnanomolarpotentselectiveallostericDNApolymerasecancerInhibitorinhibitorinhibit

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    製品名:
    ART558
    製品番号:
    HY-141520
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