A cell-permeable, orally available, phenylcyclohexyl-urea based compound that selectively downregulates the expression of p21 (~10 µM), independent of p53 expression, at either transcription or post-transcriptional level. However, it does not affect the stability of p21. Also, it has no significant effect on the activities of Raf kinases, VEGFR2 kinase, or the phosphorylation state of ERK. Effectively blocks the growth of multiple cancer cell lines (GI50 ~ 10 µM against NCI60 cell lines). Its greater inhibitory effect on cytosolic p21 is indicative of its ability to induce apoptotic cell death in 786-O cells. Synergistically suppresses the growth of HCT116 and ACHN cells in athymic nude mice when combined with imetelstat, a telomerase inhibitor (15 mg/kg of UC2288, p.o., & 30 mg/kg of imetelstat, i.p., 3 times per week).Please note that the molecular weight for this compound is batch-specific due to variable water content.
Synonyms: p21 Inhibitor, UC2288 - Calbiochem; 1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-((1r,4r)-4-(5-(trifluoromethyl)pyridin-2-yloxy)cyclohexyl)urea, trans-1-(4-Chloro-3-trifluoromethyl-phenyl)-3-(4-hydroxy-cyclohexyl)-urea, p21/Cip1/CKI/Waf1 Inhibitor, t-CTTU; UC-2288
Molecular Formula: C20H18ClF6N3O2
Molecular Weight: 481.82
Linear Structural Formula: C20H18ClF6N3O2
Purity: >=98% (HPLC)
Biochem Physiol Actions: Cell permeable: yes
Legal Information: CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes: Gupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA111, E3062.Wettersten, H.I., et al. 2013. Cancer Biol. Ther.14, 278.