ND1-YL2

Biological Activity

ND1-YL2 is a peptide-based Degrader (PROTAC^®) 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 (K_i = 320 nM). ND1-YL2 inhibits MDA-MB-231 cell migration in vitro, and suppresses metastasis of MDA-MB-231 cells in vivo.

Src antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3389 and NBP1-19188.

PROTAC^® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Targeted degradation of transcription co-activator SRC-1 through the N-degron pathway.
   Lee et al.
   Angew.Chem.Int.Ed., 2020;59:17548

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