H1 DNA-binding region of c-Myc containing Ser to Ala, and Phe to Ala substitutions (underlined) to confer an increase in its potency to inhibit c-Myc. The N-terminus of this peptide is the Int peptide sequence derived from the third Antennapedia homeodomain, to confer cell permeability. Control for this peptide is H1-S6A,F8A c-Myc inhibibitor peptide (Prod. No. BML-P606). Inhibited cloning efficiency of MCF-7 human breast cancer cells by 90% at 10 µM (IC50=5.9 µM). In MCF-7 cells, it inhibited cell growth and induced apoptosis. In addition, at 10 µM it strongly inhibited transcription of the c-Myc regulated genes ODC and p53. The non-cell-permeable control for this peptide is H1-S6A, F8A c-Myc inhibitor peptide which lacks the N-terminal internalization sequence.
Product Details
Sequence: | Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Asn-Glu-Leu-Lys-Arg-Ala-Phe-Ala-Ala-Leu-Arg-Asp-Gln-Ile |
|
MW: | 3873.6 |
|
Source: | Synthetic. |
|
Formulation: | Lyophilized. |
|
Purity: | ≥95% (HPLC) |
|
Identity: | Determined by MS. |
|
Appearance: | White to off-white powder. |
|
Solubility: | Soluble in water. |
|
Shipping: | Blue Ice |
|
Long Term Storage: | -20°C |
|
Regulatory Status: | RUO - Research Use Only |
|
Product Literature References
Inhibition of cancer cell growth and c-Myc transcriptional activity by a c-Myc helix 1-type peptide fused to an internalization sequence: L. Giorello, et al.; Cancer Res.
58, 3654 (1998),
Abstract;
The third helix of the Antennapedia homeodomain translocates through biological membranes: D. Derossi, et al.; J. Biol. Chem.
270, 14255 (1995),
Abstract;
Interaction of the bHLH-zip domain of c-Myc with H1-type peptides. Characterization of helicity in the H1 peptides by NMR: L.J. Draeger, et al.; J. Biol. Chem.
269, 1785 (1994),
Abstract;