| Sequence | H-Arg-Leu-Ala-Ala-Ala-Ala-Leu-Leu-Pro-Pro-Thr-Glu-Gln-Asp-Leu-(S)-2-(4-pentenyl)alanine-Lys-Leu-Cha-(S)-2-(4-pentenyl)alanine-Tyr-NH2(Stapled together with a double bond between (S)-2-(4-pentenyl)alanine) |
| Sequence Single | RLAAAALLPPTEQDL-(S)-2-(4-pentenyl)alanine-KL-Cha-(S)-2-(4-pentenyl)alanine-Y-NH2(Stapled together with a double bond between (S)-2-(4-pentenyl)alanine) |
| Molecular Formula | C114H189N27O28 |
| Molecular Weight | 2385.93 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | ND1-YL2 is a peptide-based PROTAC® Degrader of steroid receptor co-activator 1 (SRC-1; also known as nuclear receptor coactivator 1, NCOA1). ND1-YL2 is composed of a stapled peptide that binds SRC-1 (YL2) joined by a linker to a tetrapeptide that binds UBR box domains. Upon ternary complex formation, SRC-1 is polyubiquitinated and subsequently degraded via the N-degron pathway. ND1-YL2 induces dose-dependent degradation of SRC-1 in the MDA-MB-231 triple negative breast cancer cell line (DC50 = 10 μM), and binds to the PAS-B domain of SRC-1 (Ki = 320 nM). ND1-YL2 inhibits MDA-MB-231 cell migration in vitro, and suppresses metastasis of MDA-MB-231 cells in vivo. PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license. |