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RBPJ inhibitor-1 is an inhibitor of recombination signal binding protein for immunoglobulin kappa J region (RBPJ; IC50 = 0.18 µM in a reporter assay).1 It also inhibits the protein-protein interaction between RBPJ and the neurogenic locus notch homolog protein 2 (Notch2) intracellular domain (NICD) and the protein-protein interaction between RBPJ and small histidine-alanine-rich protein (SHARP) in cell-free assays. RBPJ inhibitor-1 (15 µM) induces cell cycle arrest at the G2/M phase and apoptosis in UT-SCC-42B squamous cell carcinoma cells.2 It reduces tumor volume in D. rerio larvae injected with UT-SCC-42B cells when administered in the tank water at a concentration of 5 µM.
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1. Disruption of NOTCH signaling by a small molecule inhibitor of the transcription factor RBPJ. Sci. Rep. 9(1), 10811 (2019).
2. Evaluation of the anticancer activity of RIN-