cyclo-[L-(2-Amino-8-oxodecanoyl)-L-(N-methoxytryptophan)-L-isoleucyl-D-pipecolinyl] Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent, cell-permeable inhibitor of histone deacetylase (IC50= 700 pM for parasitic histone deactetylase) that also exibits antiprotozoal and potential anti-malarial properties. Inhibits HeLa cell proliferation (IC50= 50-100 nM) and induces the transcriptional activation of p21 (WAF1). Also prevents H-ras-induced invasive phenotype of MCF10A cells possibly by down-regulating MMP-2. Purity: ≥95% by HPLC. Ref.: Colletti, S.L., et al. 2001. Bioorg. Med. Chem. Lett. 11, 107. Kim, J.S., et al. 2001. Biochem. Biophys. Res. Commun. 281, 866. Andrews, K.T., et al. 2000. Int. J. Parasitol. 30, 761. Kim, M.S., et al. 2000. Cancer Lett. 157, 23. Darkin-Rattray, S.J., et al. 1996. Proc. Natl. Acad. Sci. USA 93, 13143. R: 26/27/28; S: 22-26-36/37/39-45 |