KU-57788
Based on 44 publication(s) in Google Scholar
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 503468-95-9
- Fòrmula: C25H19NO3S
- Peso molecular:413.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) KU-57788
More- Cell. 2025 Jun 26;188(13):3405-3421.e27. [Abstract]
- Nat Biotechnol. 2024 May;42(5):731-744. [Abstract]
- Cell Metab. 2021 Oct 5;33(10):2076-2089.e9. [Abstract]
- Adv Mater. 2024 Sep 9:e2410031. [Abstract]
- Nat Methods. 2024 Mar;21(3):455-464. [Abstract]
- Nat Cell Biol. 2024 Sep;26(9):1545-1557. [Abstract]
- Cancer Res. 2026 Jan 13. [Abstract]
- Nat Commun. 2025 Jul 15;16(1):6502. [Abstract]
- Nat Commun. 2025 Jan 27;16(1):1077. [Abstract]
- J Clin Invest. 2024 Oct 22:e180278. [Abstract]
- J Exp Clin Cancer Res. 2022 Apr 12;41(1):140. [Abstract]
- Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
- Cell Death Dis. 2020 Jul 30;11(7):602. [Abstract]
- Cancer Lett. 2026 May 1:645:218384. [Abstract]
- Cancer Lett. 2023 Apr 1:558:216092. [Abstract]
- Genome Biol. 2021 Aug 20;22(1):236. [Abstract]
- Cell Rep. 2025 Aug 12;44(8):116152. [Abstract]
- Cell Rep. 2024 Dec 21;44(1):115094. [Abstract]
- Cell Rep. 2023 Oct 16;42(10):113256. [Abstract]
- PLoS Biol. 2026 Feb 2;24(2):e3003621. [Abstract]
- PLoS Biol. 2021 Mar 31;19(3):e3001176. [Abstract]
- Genome Res. 2021 Mar;31(3):461-471. [Abstract]
- J Cell Biol. 2022 Nov 7;221(11):e202202100. [Abstract]
- J Cell Biol. 2021 Feb 1;220(2):e201911025. [Abstract]
- Radiother Oncol. 2024 Apr:193:110111. [Abstract]
- Cancer Biol Ther. 2026 Dec 31;27(1):2646393. [Abstract]
- Int J Mol Sci. 2025 May 3;26(9):4361. [Abstract]
- Int J Mol Sci. 2022 Jul 7;23(14):7518. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Neoplasia. 2018 Mar 28;20(5):478-488. [Abstract]
- Cell Signal. 2025 Jul:131:111709. [Abstract]
- J Cereb Blood Flow Metab. 2023 May;43(5):736-748. [Abstract]
- Mol Carcinog. 2024 Nov;63(11):2218-2236. [Abstract]
- Mol Biol Rep. 2025 Mar 22;52(1):333. [Abstract]
- Vet Microbiol. 2023 Dec:287:109897. [Abstract]
- Mutat Res Genet Toxicol Environ Mutagen. 2021 Jul;867:503372. [Abstract]
- Radiat Res. 2021 May 1;195(5):412-426. [Abstract]
- State University of New York at Stony Brook. 2026.
- bioRxiv. 2026 May 1:2026.04.28.717272. [Abstract]
- Patent. US20250288582A1.
- bioRxiv. 2023 Dec 19.
- University of Gothenburg. 2023 Jun 27.
- University of Duisburg-Essen. 2020 Jul.
Customer Validation & Images
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Flow Cytometry
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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In Vivo Imaging
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IHC
Actividad biológica
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DNA-PK 14 nM (IC50) |
mTOR 1.7 μM (IC50) |
PI3K 5.0 μM (IC50) |
CRISPR/Cas9 |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
14 μM
Compound: 2, NU7441
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Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay
Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay
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[PMID: 23855836] |
| Cortical neurone | EC50 |
1.2 μM
Compound: NU7441
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Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay
Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay
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[PMID: 30840447] |
| HeLa | EC50 |
212 nM
Compound: 2, NU7441
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Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells
Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells
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[PMID: 23855836] |
| HeLa | IC50 |
14 nM
Compound: Chemical Probe: NU7441
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Inhibition of human HeLa cell nuclear extract purified DNA-PK using p53 peptide as substrate by ELISA
Inhibition of human HeLa cell nuclear extract purified DNA-PK using p53 peptide as substrate by ELISA
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[PMID: 16707462] |
| LoVo | GI50 |
0.52 μM
Compound: Chemical Probe: NU7441
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Growth inhibition of human LoVo cells measured after 5 days by crystal violet staining based assay
Growth inhibition of human LoVo cells measured after 5 days by crystal violet staining based assay
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[PMID: 16707462] |
NU7441 (0.5 to 10 μM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. NU7441 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of NU7441 and 60Coγ IR affects DNA damage repair[2].
NU7441 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor[4].
NU7441 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 503468-95-9
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Appearance Solid
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Peso molecular 413.49
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Fòrmula C25H19NO3S
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Color White to off-white
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SMILES
O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC5=C4SC6=C5C=CC=C6
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Synonyms
NU7441
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (44)
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Journal Impact Factor
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Most Recent
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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 Biotechnol
High-efficiency transgene integration by homology-directed repair in human primary cells using DNA-PKcs inhibition. [Abstract]2024 May;42(5):731-744. PMID: 37537500 -
Cell Metab
Innate immune response orchestrates phosphoribosyl pyrophosphate synthetases to support DNA repair. [Abstract]2021 Oct 5;33(10):2076-2089.e9. PMID: 34343500
KU-57788 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Oct 5;33(10):2076-2089.e9. [Abstract]
FHs 74 Int cells with expression of FLAG-TBK1 were pretreated with NU7441 (1 μM), KU55933 (10 μM),or AZD6738 (2μM) for 2h, and then exposed to 10 Gy ionizing radiation. Immunoprecipitation analyses with anti-FLAG M2 agarose beads were performed 30 min after irradiation.
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Adv Mater
A Nucleophilicity-Engineered DNA Ligation Blockade Nanoradiosensitizer Induces Irreversible DNA Damage to Overcome Cancer Radioresistance. [Abstract]2024 Sep 9:e2410031. PMID: 39246208 -
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Nat Cell Biol
2024 Sep;26(9):1545-1557. PMID: 38997456 -
Cancer Res
Inhibition of mTOR Enhances the Efficacy of Proteasome-Dependent Targeted Protein Degradation Approaches. [Abstract]2026 Jan 13. PMID: 41529091 -
Nat Commun
2025 Jul 15;16(1):6502. PMID: 40664653 -
Nat Commun
2025 Jan 27;16(1):1077. PMID: 39870664 -
J Clin Invest
DNA-PK inhibition enhances neoantigen diversity and increases T cell responses to immunoresistant tumors. [Abstract]2024 Oct 22:e180278. PMID: 39436696
KU-57788 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22:e180278. [Abstract]
The tumor cell line was treated with DMSO or DNA-PKi (2 μM NU7441) for 48 hours, at which point the drug was washed off prior to coculturing with TILs at a 1:1 ratio for 18 hours. Cytotoxicity was determined by annexin V staining with flow cytometric gating on tumor cells (based on light scatter and CD3–) and viability dye.
KU-57788 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22:e180278. [Abstract]
B16-F10 melanoma cells were treated with 2 μM NU7441 or DMSO control for 72 hours, at which point gradual darkening was observed.
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J Exp Clin Cancer Res
Flap endonuclease 1 and DNA-PKcs synergistically participate in stabilizing replication fork to encounter replication stress in glioma cells. [Abstract]2022 Apr 12;41(1):140. PMID: 35414100 -
Adv Sci (Weinh)
TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]2024 Jun 3:e2400023. PMID: 38828688
KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
NU7441 (0-2 μM; 24 h). Morphological changes of NHA/HRasV12/TRIM24 cells treated with NU7441 for 24 h at indicated concentrations.
KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
NU7441 (20 mg/kg; ip). Representative bioluminescent (BLI) images of treated animals on day 10.
KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
NU7441 (20 mg/kg; ip). Representative images showing H&E and IHC staining of brain cross sections of NHA/HRasV12/TRIM24‐derived tumors from animals treated with NU7441 or vehicle for 7 days.
KU-57788 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 3:e2400023. [Abstract]
NU7441 (0.01-100 μM; 48 h). Viability of NHA/HRasV12 cells with or without ectopic expression of TRIM24 at 48 h after treatment with NU7441.
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Cell Death Dis
Inhibition of miR-1193 leads to synthetic lethality in glioblastoma multiforme cells deficient of DNA-PKcs. [Abstract]2020 Jul 30;11(7):602. PMID: 32732911 -
Cancer Lett
GPI inactivation mediates pentose phosphate pathway flux switch-on inducing temozolomide resistance in glioma stem cell. [Abstract]2026 May 1:645:218384. PMID: 41763452 -
Cancer Lett
N6-methyadenosine modified SUV39H2 regulates homologous recombination through epigenetic repression of DUSP6 in gastric cancer. [Abstract]2023 Apr 1:558:216092. PMID: 36806557 -
Genome Biol
Effective control of large deletions after double-strand breaks by homology-directed repair and dsODN insertion. [Abstract]2021 Aug 20;22(1):236. PMID: 34416913 -
Cell Rep
53BP1 regulates p53-E2F7-dependent transcriptional gene repression and participates in the Fanconi anemia pathway. [Abstract]2025 Aug 12;44(8):116152. PMID: 40811062 -
Cell Rep
The N-degron pathway mediates the autophagic degradation of cytosolic mitochondrial DNA during sterile innate immune responses. [Abstract]2024 Dec 21;44(1):115094. PMID: 39709605 -
Cell Rep
Differential DNA damage repair and PARP inhibitor vulnerability of the mammary epithelial lineages. [Abstract]2023 Oct 16;42(10):113256. PMID: 37847590 -
PLoS Biol
DNA damage induced by HIV-1 Vpr triggers epigenetic remodeling and transcriptional programs to enhance virus transcription and latency reactivation. [Abstract]2026 Feb 2;24(2):e3003621. PMID: 41628238 -
PLoS Biol
Loss of the abasic site sensor HMCES is synthetic lethal with the activity of the APOBEC3A cytosine deaminase in cancer cells. [Abstract]2021 Mar 31;19(3):e3001176. PMID: 33788831 -
Genome Res
2021 Mar;31(3):461-471. PMID: 33574136 -
J Cell Biol
Non-catalytic allostery in α-TAT1 by a phospho-switch drives dynamic microtubule acetylation. [Abstract]2022 Nov 7;221(11):e202202100. PMID: 36222836 -
J Cell Biol
2021 Feb 1;220(2):e201911025. PMID: 33404607 -
Radiother Oncol
DNA-dependent protein kinase regulates cytosolic double-stranded DNA secretion from irradiated macrophages to increase radiosensitivity of tumors. [Abstract]2024 Apr:193:110111. PMID: 38286241 -
Cancer Biol Ther
2026 Dec 31;27(1):2646393. PMID: 41876459 -
Int J Mol Sci
CRISPR/Cas9 Ribonucleoprotein Delivery Enhanced by Lipo-Xenopeptide Carriers and Homology-Directed Repair Modulators: Insights from Reporter Cell Lines. [Abstract]2025 May 3;26(9):4361. PMID: 40362595 -
Int J Mol Sci
Chloroquine-Induced DNA Damage Synergizes with Nonhomologous End Joining Inhibition to Cause Ovarian Cancer Cell Cytotoxicity. [Abstract]2022 Jul 7;23(14):7518. PMID: 35886866 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Neoplasia
Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. [Abstract]2018 Mar 28;20(5):478-488. PMID: 29605721 -
Cell Signal
2025 Jul:131:111709. PMID: 40037423 -
J Cereb Blood Flow Metab
Activin A alleviates neuronal injury through inhibiting cGAS-STING-mediated autophagy in mice with ischemic stroke. [Abstract]2023 May;43(5):736-748. PMID: 36537048 -
Mol Carcinog
Pyroptosis-related gene GSDMC indicates poor prognosis and promotes tumor progression by activating the AKT/mTOR pathway in lung squamous cell carcinoma. [Abstract]2024 Nov;63(11):2218-2236. PMID: 39136610 -
Mol Biol Rep
p53-deficient cancer cells hyperactivate DNA double-strand break repair pathways to overcome chemotherapeutic damage and augment survival. [Abstract]2025 Mar 22;52(1):333. PMID: 40119972 -
Vet Microbiol
Porcine IGFBP3 promotes porcine circovirus type 2 replication via PERK/eIF2α mediated DNA damage. [Abstract]2023 Dec:287:109897. PMID: 37922860 -
Mutat Res Genet Toxicol Environ Mutagen
Analysis of chromatid-break-repair detects a homologous recombination to non-homologous end-joining switch with increasing load of DNA double-strand breaks. [Abstract]2021 Jul;867:503372. PMID: 34266628 -
Radiat Res
Nucleoside Analogs Radiosensitize G0 Cells by Activating DNA End Resection and Alternative End-Joining. [Abstract]2021 May 1;195(5):412-426. PMID: 33755161 -
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bioRxiv
2026 May 1:2026.04.28.717272. PMID: 42094395 -
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Solvente y solubilidad
DMSO : 6.67 mg/mL (16.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
HepG2 cells (4000 per well) are cultured in a 96-well plate for 24 h. Once the cells complete the attachment, 0.1 µM, 1 µM, 5 µM, and 10 µM of KU-57788 are added to the culture media. After 12 h of KU-57788 treatment, 10% CCK-8 solution is added into the culture media, and the incubation continued for two h. OD450 values are determined by a spectrometer, and the results are analyzed to measure the cell growth.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (290 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Justin J J Leahy, et al. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. [Content Brief]
[2]. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905 [Content Brief]
[3]. Hardcastle IR, et al. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. J Med Chem. 2005 Dec 1;48(24):7829-46 [Content Brief]
[4]. Ember SW, et al. The acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem Biol. 2014 Feb 25. [Content Brief]
[5]. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93 [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4184 mL | 12.0922 mL | 24.1844 mL | 60.4610 mL |
| 5 mM | 0.4837 mL | 2.4184 mL | 4.8369 mL | 12.0922 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4184 mL | 6.0461 mL | |
| 15 mM | 0.1612 mL | 0.8061 mL | 1.6123 mL | 4.0307 mL |
KU-57788 Related Classifications
HY-11006 Related Classifications
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