STL127705

STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC 50 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 apoptosisIn VitroSTL127705 (Compound L) (0-100 µM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase. antiproliferative activity (0-100 µM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells. STL127705 (0-40 µM; 6h) shows antiproliferative activity in a dose dependent manner. TL127705 (1 µM; 48 h) significantly promotes apoptotic when combination with gemcitabine. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: SF-767, PrEC cells Concentration: 0-40 µM Incubation Time: 6 h Result: Showed cytotoxicity in a dose dependent manner. Western Blot AnalysisCell 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 AnalysisCell 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.Form:Solid

Specifications & Purity: STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC 50 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 apoptosisIn VitroSTL127705 (Compound L) (0-100 µM) inhibits binding of Ku70/80 to a DNA substrate and inhibits Ku-dependent activation of the DNA-PKCS kinase. antiproliferative activity (0-100 µM; 6h) decreases the expression of DNA-PKCS auto-phosphorylation in SF-767 cells. STL127705 (0-40 µM; 6h) shows antiproliferative activity in a dose dependent manner. TL127705 (1 µM; 48 h) significantly promotes apoptotic when combination with gemcitabine. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: SF-767, PrEC cells Concentration: 0-40 µM Incubation Time: 6 h Result: Showed cytotoxicity in a dose dependent manner. Western Blot AnalysisCell 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 AnalysisCell 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.Form:Solid

Grade: Moligand™

Molecular Formula: C22H20FN5O4

Molecular Weight: 437.42

PubChem CID: 53333307

Isomeric SMILES: COC1=C(C=C(C=C1)CCNC2=NC=C3C(=N2)NC(=O)N(C3=O)C4=CC(=CC=C4)F)OC

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads

UPC:

51373426

Weight:

1.09 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

S646275-1mg

Country of Origin:

China

CAS:

1326852-06-5

Product Size:

1mg

Harmonized Tariff Code:

2931.90.90