1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. DNA-PK Apoptosis
  3. STL127705

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.

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STL127705 Chemical Structure

STL127705 Chemical Structure

CAS No. : 1326852-06-5

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Based on 4 publication(s) in Google Scholar

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Description

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[1][2].

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.

Cell Viability Assay[1]

Cell Line: SF-767, PrEC cells
Concentration: 0-40 µM
Incubation Time: 6 h
Result: Showed cytotoxicity in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: SF-767 cells
Concentration: 0-100 µM
Incubation Time: pre-treated for 2 h and then co-incubation 4 h
Result: Decreased the DNA-PKCS autophosphorylation but total DNA-PKCS was not suppressed by STL127705.

Apoptosis Analysis[1]

Cell Line: H1299 cells
Concentration: 1 µM
Incubation Time: 48 h
Result: Induced apoptosis with apoptosis rate significantly increased to 76% when treated with STL127705 in combination with gemcitabine.
Molecular Weight

437.42

Formula

C22H20FN5O4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC2=NC(NCCC3=CC=C(OC)C(OC)=C3)=NC=C2C(N1C4=CC=CC(F)=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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.

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STL127705 Related Classifications

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.

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Product Name:
STL127705
Cat. No.:
HY-122727
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