ND1-YL2

Pricing Availability   Qty
Cat.No. 7388 - ND1-YL2 | 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 (double bond covalent bridge: X-16-X-20)
Description: SRC-1 peptide-based PROTAC®; active in vivo
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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.

Licensing Information

Sold under license from Pohang University of Science and Technology

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

Storage Store at -20°C
Purity ≥95% (HPLC)
InChI Key CWOOYUYOHKVUNB-BHZFBJKQSA-N
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

Solubility Soluble to 1 mg/ml in water

References

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.

Keywords: ND1-YL2, ND1-YL2 supplier, stapled, peptide, degraders, protacs, degrades, SRC1, NCOA1, steroid, receptor, co-activator, 1, nuclear, coactivator, UBR, box, domain, N-end, rule, N-degron, pathway, targeted, protein, degradation, Active, Degraders, Other, Nuclear, Receptors, 7388, Tocris Bioscience

Citations for ND1-YL2

Citations are publications that use Tocris products.

Currently there are no citations for ND1-YL2. Do you know of a great paper that uses ND1-YL2 from Tocris? Please let us know.

Reviews for ND1-YL2

There are currently no reviews for this product. Be the first to review ND1-YL2 and earn rewards!

Have you used ND1-YL2?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Epigenetics

Epigenetics Scientific Review

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

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, 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

Targeted Protein Degradation Poster

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