Bcl-2 Converter, D-NuBCP-9-r8, Cell-permeable - Calbiochem

An all-D-amino acid version of the Nur77-derived minimum Bcl-2/Bcl-B/Bfl-1-conformation converting sequence is conjugated with a D-Arg octamer to facilitate its cellular delivery. CD binding studies reveal a 1:1 stoichiometric binding and that Bcl-2 unstructured loop region (aa 29-90) as the main D-NuBCP-9 interacting site with possible additional involvement of the BH4 domain. D-NuBCP-9-induced apoptosis is Bcl-2-dependent (100% vs 0% inhibition, respectively, of MEF vs Bcl-2^-/- MEF colonies formation by 15 µM D-NuBCP-9) and requires the presence of either Bak or Bax (0% inhibition of Bax^-/-Bak^-/- MEF colonies formation). D-NuBCP-9-induced apoptosis in HeLa cultures is also demonstrated to be potentiated by 114% and 78%, respectively, upon vector expression of Bcl-B or Bfl-1. When applied to MDA-MB435-xenografted mice on the 10th & 13th day after cancer cell implant, D-NuBCP-9 (620 µg/mouse) reportedly suppressed tumor growth (by 80% on day 55) by inducing cancer cell apoptosis in vivo.

Packaged under inert gas

Supplied as a trifluoroacetate salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

(D)-Ac-phe-ser-arg-ser-leu-his-ser-leu-leu-Gly-NH-(CH₂)₅-CO-arg-arg-arg-arg-arg-arg-arg-arg-NH₂

Kolluri, S.K., et al. 2008. Cancer Cell14, 285.

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Toxicity: Standard Handling (A)