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Description: SRC-1 peptide-based Degrader (PROTAC®); active in vivo
Purity: ≥95% (HPLC)
Literature (4)

Biological Activity for ND1-YL2

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 (Ki = 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.

Licensing Information

Sold under license from Pohang University of Science and Technology

Technical Data for ND1-YL2

M. Wt 2385.93
Formula C114H189N27O28

(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

Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2582803-80-1
Smiles N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N1[C@H](C(N2[C@H](C(NC([C@@H](C)O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@]3(C)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CC4CCCCC4)C(N[C@](CCC/C=C\CCC3)(C)C(N[C@@H](CC5=CC=C(O)C=C5)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC2)=O)CCC1)=O)=O)=O)=O)=O)=O)=O)=O

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.

Solubility Data for ND1-YL2

Solubility Soluble to 1 mg/ml in water

References for ND1-YL2

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for ND1-YL2, please let us know.

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Citations for ND1-YL2

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Targeted Protein Degradation Research Product Guide

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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

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This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation Poster

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Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia