Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetBcl-2

Target IC₅₀: 130 nM against Bcl-2

Cell permeable: yes

General description

A cell-permeable Bcl-2 binding peptide that induces apoptosis in Bcl-2 expressing cells with no apparent effect on normal peripheral lymphocytes. Also reported to diminish the growth of human myeloid leukemia in severe combined immunodeficient mice. The peptide is derived from the BH3 domain (residues 140-165, a death domain) of Bad and is modified to be cell-permeable by attaching a decanoyl moiety at the N-terminus.

A cell-permeable peptide that binds to Bcl-2 with high affinity (IC₅₀ = 130 nM in a competition binding study) and induces apoptosis. Displays antitumor activity in cells overexpressing Bcl-2 with no apparent effect on normal peripheral lymphocytes. The peptide is derived from the BH3 domain (residues 140 - 165, a “death domain”) of Bad and is modified to be cell permeant by attaching a decanoyl moiety at the N-terminus.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wang, J-L., et al. 2000. Cancer Res.60, 1498.Kelekar, A., et al. 1997. Mol. Cell. Biol.17, 7040.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 2 weeks at -20°C.

Sequence

CH₃(CH₂)₈CONH-Lys-Asn-Leu-Trp-Ala-Ala-Gln-Arg-Tyr-Gly-Arg-Glu-Leu-Arg-Arg-Met-Ser-Asp-Glu-Phe-Glu-Gly-Ser-Phe-Lys-Gly-Leu-OH

Warning

Toxicity: Standard Handling (A)