STL127705
Based on 8 publication(s) in Google Scholar
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis.
For research use only. We do not sell to patients.
- Purity : 98.97%
- CAS No.: 1326852-06-5
- Formula: C22H20FN5O4
- Molecular Weight:437.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) STL127705
More- Cell Res. 2026 Jan 7. [Abstract]
- Immunity. 2021 Apr 13;54(4):632-647.e9. [Abstract]
- Nucleic Acids Res. 2023 Dec 11;51(22):12242-12260. [Abstract]
- Adv Sci (Weinh). 2025 Jul;12(28):e2412698. [Abstract]
- Research (Wash D C). 2024 Mar 26:7:0331. [Abstract]
- Cell Rep. 2025 Jun 13;44(6):115851. [Abstract]
- Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
- Biotechnol Bioeng. 2023 Sep;120(9):2419-2440. [Abstract]
Customer Validation & Images
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WB
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WB
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WB
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Flow Cytometry
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Cell Proliferation/Viability Assay
Biological Activity
Description
IC50 & Target
IC50: 3.5 μM (Ku 70/80), 2.5 μM (DNA-PKCS)[1]
In Vitro
STL127705 (Compound L) (0-100 μM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase[1].
STL127705 (0-100 μM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells[1].
STL127705 (0-40 μM; 6h) shows antiproliferative activity in a dose dependent manner[1].
TL127705 (1 μM; 48 h) significantly promotes apoptotic when combination with gemcitabine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SF-767, PrEC cells
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Concentration:0-40 µM
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Incubation Time:6 h
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Result:Showed cytotoxicity in a dose dependent manner.
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Cell Line:SF-767 cells
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Concentration:0-100 µM
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Incubation Time:pre-treated for 2 h and then co-incubation 4 h
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Result:Decreased the DNA-PKCS autophosphorylation but total DNA-PKCS was not suppressed by STL127705.
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Cell Line:H1299 cells
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Concentration:1 µM
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Incubation Time:48 h
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Result:Induced apoptosis with apoptosis rate significantly increased to 76% when treated with STL127705 in combination with gemcitabine.
Chemical Information
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CAS No. 1326852-06-5
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Appearance Solid
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Molecular Weight 437.42
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Formula C22H20FN5O4
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Color Off-white to light yellow
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SMILES
O=C1NC2=NC(NCCC3=CC=C(OC)C(OC)=C3)=NC=C2C(N1C4=CC=CC(F)=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell Res
Sensing of DNA double-strand breaks by the NHEJ system stabilizes RORγt transcriptional activity and shapes Th17 pathogenicity in autoimmunity. [Abstract]2026 Jan 7. PMID: 41495483
STL127705 purchased from MedChemExpress. Usage Cited in: Cell Res. 2026 Jan 7. [Abstract]
Immunoblot for pSer2056-DNA-PKcs expression in HP Th17 transfected with FLAG-IER2, with or without STL127705 (1 μmol/L).
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Immunity
Cytoplasmic DNA sensing by KU complex in aged CD4+ T cell potentiates T cell activation and aging-related autoimmune inflammation. [Abstract]2021 Apr 13;54(4):632-647.e9. PMID: 33667382 -
Nucleic Acids Res
The RNA-binding motif protein 14 regulates telomere integrity at the interface of TERRA and telomeric R-loops. [Abstract]2023 Dec 11;51(22):12242-12260. PMID: 37930826
STL127705 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 Dec 11;51(22):12242-12260. [Abstract]
Dot blot analysis of telomere DNA contents in the indicated ChIP and input from U2OS cells treated with either 1 μM Olaparib (OLP) or 2 μM STL127705 (STL) for 24 h. IgG ChIP served as a negative control. The telomeric repeat signal was detected using the Telo-C-Biotin (CCCTAA)4 probe.
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Adv Sci (Weinh)
DNA-PKcs-Driven YAP1 Phosphorylation and Nuclear Translocation: a Key Regulator of Ferroptosis in Hyperglycemia-Induced Cardiac Dysfunction in Type 1 Diabetes. [Abstract]2025 Jul;12(28):e2412698. PMID: 40279648 -
Research (Wash D C)
DNA-PKcs Phosphorylates Cofilin2 to Induce Endothelial Dysfunction and Microcirculatory Disorder in Endotoxemic Cardiomyopathy. [Abstract]2024 Mar 26:7:0331. PMID: 38550779 -
Cell Rep
ENPP1 governs the metabolic regulation of effector T cells in autoimmunity by detecting cytosolic mitochondrial DNA. [Abstract]2025 Jun 13;44(6):115851. PMID: 40516055 -
Eur J Med Res
RHBDD1 induces cell cycle arrest in TP53-mutant NSCLC cells by promoting endoplasmic reticulum-associated degradation of p53 and DNA-PKcs. [Abstract]2025 Sep 26;30(1):859. PMID: 41013641
STL127705 purchased from MedChemExpress. Usage Cited in: Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
Levels of RHBDD1, DNA-PKcs, and p53 proteins in sh-RHBDD1-transfected A549 cells treated with the DNA-PKcs inhibitor STL127705 (3.5 μM).
STL127705 purchased from MedChemExpress. Usage Cited in: Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
Levels of RHBDD1, DNA-PKcs and p53 in sh-RHBDD1 transfected NCI-H596 cells treated with STL127705 (3.5 μM).
STL127705 purchased from MedChemExpress. Usage Cited in: Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
Cell cycle analysis of transfected NCI-H596 cells co-treated with STL127705 (3.5 μM) or Nutlin-3a for 48 h by flow cytometry.
STL127705 purchased from MedChemExpress. Usage Cited in: Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
Viability of transfected NCI-H596 cells co-treated with STL127705 (3.5 μM) or Nutlin-3a for 48 h.
STL127705 purchased from MedChemExpress. Usage Cited in: Eur J Med Res. 2025 Sep 26;30(1):859. [Abstract]
ERAD marker analysis in sh-RHBDD1- or pcDNA-RHBDD1-transfected cells treated with STL127705 (3.5 μM) or Nutlin-3a, assessed by western blotting.
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Biotechnol Bioeng
High-efficiency and multilocus targeted integration in CHO cells using CRISPR-mediated donor nicking and DNA repair inhibitors. [Abstract]2023 Sep;120(9):2419-2440. PMID: 37039773
Solvent & Solubility
In Vitro:
H2O : < 0.1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
* STL127705 is usually formulated as a suspension.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (273 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Weterings E, et al. A novel small molecule inhibitor of the DNA repair protein Ku70/80. DNA Repair (Amst). 2016 Jul;43:98-106. [Content Brief]
[2]. Guo N, et al. Inhibiting nonhomologous end-joining repair would promote the antitumor activity of gemcitabine in nonsmall cell lung cancer cell lines. Anticancer Drugs. 2022 Jun 1;33(5):502-508. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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