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197320 Sigma-Aldrich

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.

Synonym: (D)-Ac-fsrslhsll-G-NH(CH₂)₅-CO-rrrrrrrr-NH₂, D-NuBCP-9, (D)-Ac-fsrslhsll-G-NH(CH₂)₅-CO-rrrrrrrr-NH₂, D-NuBCP-9

  • Empirical Formula (Hill Notation) C106H191N49O23

  • Molecular Weight 2519.97

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Properties

Related Categories Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology More...
brand family   Calbiochem
feature productdata solubility   H₂O (1 mg/ml) or DMSO (5 mg/ml)
form   Lyophilized solid
packaging   2 mg in Plastic ampoule (197320-2MG)
purity   ≥95% by HPLC
shipped in   ambient
storage conditions   +2C to +8C
  Hygroscopic
  Ok to freeze

Description

General description

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.

Other Notes

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

Packaging

Packaged under inert gas

Reconstitution

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

Warning

Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Sequence

(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

Safety & Documentation

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