製品番号: HY-141520

ART558

50 Cited Publications

カスタマーレビュー

Based on 50 publication(s) in Google Scholar

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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純度: 99.75%
CAS 番号: 2603528-97-6
分子式: C₂₁H₂₁F₃N₄O₂
分子量:418.41

保管条件:

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

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

ART558 構造式

CAS 番号: 2603528-97-6

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (50)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
Bioz

生物活性

製品説明

IC₅₀ & Target

DNA Polymerase

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

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	EC₅₀	>12 μM Compound: 22; ART558	Antiproliferative activity against human DLD-1 cells Antiproliferative activity against human DLD-1 cells	[PMID: 36200480]
DLD-1	EC₅₀	0.8 nM 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]
HEK293	EC₅₀	180 nM 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; BRCA2^wild-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; BRCA2^wild-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.

Cell Viability Assay^[1]

Cell Line:

BRCA2^wild-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:

BRCA2^wild-type or BRCA2^‒/‒ cells
Concentration:

5μM
Incubation Time:

0~72 hours
Result:

Showed γH2AX accumulation in cells.

化学情報

CAS 番号 2603528-97-6
性状 Solid
分子量 418.41
分子式 C₂₁H₂₁F₃N₄O₂
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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Publications (50)

All Flow CytometryBio/Physico-chemical AssayWBCell Proliferation/Viability Assay

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Journal Impact Factor

Science

Different repair pathways support intact or truncated insertions by R2 retrotransposon protein. [Abstract]

2026 Feb 26;391(6788):eadz3121. PMID: 41231928
Cell

Extrachromosomal DNA replication and maintenance couple with DNA damage pathway in tumors. [Abstract]

2025 Jun 26;188(13):3405-3421.e27. PMID: 40300601
Nat Methods

Efficient high-precision homology-directed repair-dependent genome editing by HDRobust. [Abstract]

2023 Sep;20(9):1388-1399. PMID: 37474806
Nat Cell Biol

Transcription-coupled DNA-protein crosslink repair by CSB and CRL4CSA-mediated degradation. [Abstract]

2024 May;26(5):770-783. PMID: 38600236
Nat Commun

EP300 deficiency leads to chronic replication stress mediated by defective replication fork protection. [Abstract]

2025 Dec 7. PMID: 41354653

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.
Nat Commun

Unveiling the cut-and-repair cycle of designer nucleases in human stem and T cells via CLEAR-time dPCR. [Abstract]

2025 Nov 3;16(1):9571. PMID: 41184307

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.
Nat Commun

Polymerase theta repairs persistent G1-induced DNA breaks in S-phase during class switch recombination. [Abstract]

2025 Nov 26;16(1):10536. PMID: 41298353
Nat Commun

Refined DNA repair manipulation enables a universal knock-in strategy in mouse embryos. [Abstract]

2025 Jul 15;16(1):6502. PMID: 40664653
Nat Commun

HR eye & MMR eye: one-day assessment of DNA repair-defective tumors eligible for targeted therapy. [Abstract]

2025 May 12;16(1):4239. PMID: 40355434
Nat Commun

Replication stress induces POLQ-mediated structural variant formation throughout common fragile sites after entry into mitosis. [Abstract]

2024 Nov 6;15(1):9582. PMID: 39505880

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.
Nat Commun

PARG is essential for Polθ-mediated DNA end-joining by removing repressive poly-ADP-ribose marks. [Abstract]

2024 Jul 11;15(1):5822. PMID: 38987289
Nat Commun

ATM inhibition exploits checkpoint defects and ATM-dependent double strand break repair in TP53-mutant glioblastoma. [Abstract]

2024 Jun 21;15(1):5294. PMID: 38906885
Nat Commun

Polymerase θ inhibition activates the cGAS-STING pathway and cooperates with immune checkpoint blockade in models of BRCA-deficient cancer. [Abstract]

2023 Mar 13;14(1):1390. PMID: 36914658

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.
J Clin Invest

POLQ inhibition elicits an immune response in homologous recombination-deficient pancreatic adenocarcinoma via cGAS/STING signaling. [Abstract]

2023 Jun 1;133(11):e165934. PMID: 36976649

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.
Nucleic Acids Res

PARP1 and PARP2 are dispensable for DNA repair by microhomology-mediated end-joining at double-ended DSBs. [Abstract]

2026 Jan 5;54(1):gkaf1437. PMID: 41495903
Nucleic Acids Res

Single-stranded DNA with internal base modifications mediates highly efficient knock-in in primary cells using CRISPR-Cas9. [Abstract]

2024 Nov 21:gkae1069. PMID: 39569586
Nucleic Acids Res

Novel BRCA1-PLK1-CIP2A axis orchestrates homologous recombination-mediated DNA repair to maintain chromosome integrity during oocyte meiosis. [Abstract]

2024 Dec 9:gkae1207. PMID: 39657788
Cell Rep Med

Polθ activity modulates sensitivity to standard therapies in DNMT3A-deficient leukemia. [Abstract]

2026 Mar 17;7(3):102687. PMID: 41850232
Proc Natl Acad Sci U S A

HPV16 E6 oncoprotein promotes microhomology-mediated viral integration by increasing PolΘ protein expression. [Abstract]

2026 Mar 10;123(10):e2532479123. PMID: 41785316
Genes Dev

WRN exonuclease imparts high fidelity on translesion synthesis by Y family DNA polymerases. [Abstract]

2024 Apr 17;38(5-6):213-232. PMID: 38503516
J Transl Med

Polymerase theta inhibition impairs tumor growth and amplifies melphalan-induced DNA damage in multiple myeloma. [Abstract]

2025 Oct 10;23(1):1079. PMID: 41074018
Cell Rep

Fanconi anemia-associated chromosomal radial formation is dependent on POLθ-mediated alternative end joining. [Abstract]

2023 Apr 21;42(5):112428. PMID: 37086407
Int J Mol Sci

Polθ Inhibitor (ART558) Demonstrates a Synthetic Lethal Effect with PARP and RAD52 Inhibitors in Glioblastoma Cells. [Abstract]

2024 Aug 23;25(17):9134. PMID: 39273083
DNA Repair

Contributions of DNA double strand break repair pathways to DNA crosslink repair. [Abstract]

2025 Sep:153:103889. PMID: 40913914
Surgery

Overexpression of human DNA polymerase theta is a biomarker of aggressive and DNA repair-deficient papillary thyroid cancers. [Abstract]

2024 Jun 18:S0039-6060(24)00303-9. PMID: 38897886
Gene

Inhibition of p300 Increases Cytotoxicity of Cisplatin in Pancreatic Cancer Cells. [Abstract]

2023 Dec 20:888:147762. PMID: 37666373
Pathologie (Heidelb)

POLQ and DNA-PK inhibition in muscle-invasive bladder cancer : Enhancing radiosensitivity with novel DNA damage response inhibitors to improve radiotherapy outcomes. [Abstract]

2025 Nov 26. PMID: 41295990
bioRxiv

2026 Apr 9.
bioRxiv

2026 Feb 17.
bioRxiv

2026 Feb 21.
bioRxiv

Synthetic Hybrid Receptors for Safer and Programmable T Cell Therapy. [Abstract]

2026 Jan 23:2026.01.22.701150. PMID: 41648153
bioRxiv

2025 Nov 30.
bioRxiv

2025 Nov 20.
bioRxiv

Defective Microhomology-Mediated End-joining in SMARCB1-Deficient Tumors. [Abstract]

2025 Nov 21:2025.11.20.689563. PMID: 41332615
bioRxiv

2025 Sep 11.
bioRxiv

2025 Sep 21.
Patent

US20250236892A1.
bioRxiv

PARP1 and PARP2 are dispensable for DNA repair by microhomology-mediated end-joining during mitosis. [Abstract]

2025 Jun 9:2025.06.09.658719. PMID: 40661535
bioRxiv

Disruption of Microhomology-mediated End-joining in Ewing Sarcoma. [Abstract]

2025 May 10:2025.05.06.651696. PMID: 40568108
Technische Universitat Darmstadt

2025 May 8.
bioRxiv

2025 January 24.
bioRxiv

DNA polymerase theta-mediated DNA repair is a functional dependency and therapeutic vulnerability in DNMT3A deficient leukemia cells. [Abstract]

2024 Sep 19:2024.09.15.613155. PMID: 39411165
bioRxiv

DNA-PKcs Inhibition Improves Sequential Gene Insertion of the Full-Length CFTR cDNA in Airway Stem Cells. [Abstract]

2024 Aug 12:2024.08.12.607571. PMID: 39185207
Res Sq

2024 Jun 25.
biorxiv

2024 May 29.
bioRxiv

2024 Apr 25.
bioRxiv

Single-Stranded DNA with Internal Base Modifications Mediates Highly Efficient Gene Insertion in Primary Cells. [Abstract]

2024 Feb 1:2024.02.01.578476. PMID: 38352420
bioRxiv

Non-homologous end joining shapes the genomic rearrangement landscape of chromothripsis from mitotic errors. [Abstract]

2023 Aug 11:2023.08.10.552800. PMID: 37609143
bioRxiv

2023 Jun 29.
Res Sq

Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells. [Abstract]

2023 Apr 6:rs.3.rs-2688694. PMID: 37066268

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

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

Mass

濃度

体積

分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始)

体積 _(開始)

濃度 _(終了)

体積 _(終了)

体内:

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

Stock Solution Working Solution

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.

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Zatreanu D, et al. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance. Nat Commun. 2021 Jun 17;12(1):3636. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

50 Cited Publications

100 mg お問い合わせ

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ART558

MCE Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 ART558

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (50)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ART558

MCE Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 ART558

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (50)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

ART558 関連分類

製品番号: HY-141520