Ku-0063794, 5 mg

From STEMCELL Technologies, this small molecule is a cell-permeable, selective inhibitor of the serine-threonine kinase mammalian target of rapamycin (mTOR). The compound inhibits both the mTORC1 and mTORC2 complexes with an IC50 of 10 nM and shows > 1000-fold specificity against 76 other protein kinases or 7 lipid kinases, including PI3 kinases (García-Martínez et al.). It is supplied as a crystalline solid with a molecular weight of 465.5 g/mol and a purity of ≥ 98%. The product is stable at -20°C for 12 months from the date of receipt and should be protected from prolonged exposure to light. Stock solutions can be prepared in DMSO at concentrations up to 4 mM; the compound has low solubility in aqueous media.

Published applications include extending the lifespan of Toll-like receptor-activated dendritic cells by preserving mitochondrial oxidative phosphorylation (Amiel et al.) and inhibiting cell growth via G1-cell cycle arrest in mouse embryonic fibroblasts and human non-small cell lung carcinoma cell lines (Fei et al.; García-Martínez et al.). Additional studies report inhibition of tumor growth in a xenograft model of renal cell carcinoma (Zhang et al.) and reduction of keloid volume in an ex vivo organ culture model, along with inhibition of keloid cell spreading, proliferation, migration, and invasive properties in vitro (Syed et al.).