SRC-1 peptide-based PROTAC™; active in vivo
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. This Degrader 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
.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-054889 |
| Réf. fabricant | 18739566 |
| Pureté | 95% |
| Contenu et stockage | Store at -20°C |
| Poids moléculaire | M.W.-observed: 2385.93 |
| Quantité | 100 μg |
