197320
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(s):
Bcl-2 Converter, D-NuBCP-9-r8, Cell-permeable - Calbiochem, (D)-Ac-fsrslhsll-G-NH(CH₂)₅-CO-rrrrrrrr-NH₂, D-NuBCP-9
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About This Item
Empirical Formula (Hill Notation):
C106H191N49O23
Molecular Weight:
2519.97
UNSPSC Code:
12352200
Quality Level
Assay
≥95% (HPLC)
form
lyophilized solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
solubility
water: 1 mg/mL
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
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.
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
(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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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