UC2288

UC2288 is an inhibitor of cyclin-dependent kinase inhibitor (p21^WAF1), a negative regulator of cell cycle progression.¹ It reduces the protein levels and mRNA expression of p21^WAF1 independently of Raf and p53, respectively, when used at a concentration of 10 µM. UC2288 (8 µM) decreases the proliferation of, and phosphorylation of EGFR and extracellular-signal-related kinases 1/2 (ERK1/2) in, CNE-2 and 5-8F nasopharyngeal cell lines.² In vivo, UC2288, in combination with the telomerase inhibitor imetelstat, reduces tumor growth and induces apoptosis in an HCT116 colorectal cancer mouse xenograft model when administered at a dose of 15 mg/kg three times per week.³

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1. Wettersten, H.I., Hwang, S.H., Li, C., et al. A novel p21 attenuator which is structurally related to sorafenib. Cancer Biol. Ther. 14(3), 278-285 (2013).

2. Liang, R., and Zhu, X. UC2288 induces cell apoptosis of nasopharyngeal carcinoma cells via inhibiting EGFR/ERK pathway. J. Cancer 12(4), 988-995 (2021).

3. Gupta, R., Dong, Y., Solomon, P.D., et al. Synergistic tumor suppression by combined inhibition of telomerase and CDKN1A. Proc. Natl. Acad. Sci. USA 111(30), E3062-E3071 (2014).