KU0060648, 25mg

STEMCELL Technologies supplies KU0060648, a small molecule classified as an NHEJ pathway inhibitor. It acts as an ATP-competitive and highly potent inhibitor of DNA-dependent protein kinase (DNA-PK), with reported IC₅₀ values of 19 nM in MCF7 human breast cancer cells and 170 nM in SW620 human colon cancer cells. The compound also inhibits phosphoinositide 3-kinase (PI3K), with IC₅₀ values of 39 nM in MCF7 cells and greater than 10 µM in SW620 cells, suggesting a cell-dependent mechanism.

The chemical name is 2-(4-ethylpiperazin-1-yl)-N-[4-(2-morpholin-4-yl-4-oxochromen-8-yl)dibenzothiophen-1-yl]acetamide. The molecular formula is C₃₃H₃₄N₄O₄S with a molecular weight of 582.7 g/mol, and the CAS number is 881375-00-4. KU0060648 is supplied as a crystalline solid with a purity of at least 98%.

Published applications include genome editing, where KU0060648 reduces the frequency of non-homologous end joining (NHEJ) and increases the efficiency of homology-directed repair (HDR) in CRISPR-Cas9 workflows. In cancer research, it inhibits tumour growth and sensitises human cancer cells to DNA double-strand-break (DSB)-inducing therapies, such as chemo- or radiotherapy, by inhibiting both DNA-PK and PI3K and preventing the execution of DSB repair. The product is stable at -20°C as supplied and should be protected from prolonged exposure to light. For long-term storage it should be kept with a desiccant, and it remains stable as supplied for 12 months from the date of receipt. Solubility in DMSO is at most 1.7 mM, and the compound has low solubility in aqueous media. For cell culture use, stock solutions should be diluted into culture medium immediately before use, avoiding a final DMSO concentration above 0.1% to limit potential cell toxicity.