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Roslin-2 is a reactivator of p53.1 Roslin-2 (111, 333, and 1000 µM) impairs the interaction between focal adhesion kinase (FAK) and p53 and restores p53 transcriptional activity. It reverses FAK-mediated suppression of the expression of p53-dependent p21, MDM2, and Bax in wild-type p53 HCT116 colon and MCF-7 breast cancer cells, but not in p53 mutant SW620 colon cancer cells, when used at concentrations ranging from 1 to 50 µM. Roslin-2 (10 µM) potentiates the pro-apoptotic effect of doxorubicin (Item No. 15007) and 5-fluorouracil (Item No. 14416) in p53+/+, but not p53-/-, HCT116 cells. It reduces tumor growth and activates p21 in p53+/+, but not p53-/- tumors, in HCT116 mouse xenograft models when administered at a dose of 60 mg/kg.
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1. Disruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked tumor growth. BMC Cancer 13:342, (2013).