ND1-YL2

Catalog # Availability Size / Price Qty
7388/100U

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ND1-YL2
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Description: SRC-1 peptide-based PROTAC®; active in vivo

Purity: ≥95%

Product Details
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Biological Activity

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 in vivo.

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

Technical Data

M.Wt:
2385.93
Formula:
C114H189N27O28
Sequence:
RLAAAALLPPTEQDLXKLXXY

(Modifications: X-19 = Cha, X-16 and X-20 = (S)-2-(4-pentenyl)alanine, X-16 and X-20 stapled together with a double bond), Tyr-21 = C-terminal amide

Solubility:
Soluble to 1 mg/ml in water
Purity:
≥95%
Storage:
Store at -20°C

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

Licensing Caveats:
Sold under license from Pohang University of Science and Technology

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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