LTURM 34

LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA-PK

Signaling Pathways >> PI3K/Akt/mTOR >> DNA-PK

Research Areas >> Cancer

DNA-PK:34 nM (IC50)

PI3Kβ:5.8 μM (IC50)

PI4Kδ:8.5 μM (IC50)

LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 shows potent and broad ranging antiproliferative activity. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line[1].

LTURM34 is dissolved at 10 mM in DMSO and stored at -20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES pH 7.5, 5 mM MgCl2 with 180 μM PI and 10 μM ATP. After a 60 min incubation at room temperature the reaction is stopped by the addition of 50 μl of Kinase-Glo followed by a further 15 min incubation. Luminescence is then read using a luostar plate reader. LTURM34 is diluted in 20% (v/v) DMSO at the ndicated concentrations in order to generate a concentration versus inhibition of enzyme activity curve which is then analysed using GraphPad Prism version 5.00 for Windows, in order to calculate the IC50[1].

[1]. Morrison R, et al. Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines. Eur J Med Chem. 2016 Mar 3;110:326-39.

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