RO4929097 is a potent and selective small molecule inhibitor of γ-secretase (IC50=4nM), producing inhibitory activity of Notch signaling in tumor cells. It inhibits Notch processing in tumor cells as measured by the reduction of intracellular Notch expression by Western blot. This leads to reduced expression of the Notch transcriptional target gene Hes1. RO4929097 does not block tumor cell proliferation or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype. Current it is in phase I study in patients with advanced solid tumors.

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NOTE: Under licensing agreement with Hoffmann-La Roche Ltd, this product is to be used for in vitro study only.