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Submit ReviewND1-YL2
Description: SRC-1 peptide-based Degrader (PROTAC®); active in vivo
Purity: ≥95% (HPLC)
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 |
| 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) |
| CAS Number | 2582803-80-1 |
| 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 for ND1-YL2
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for ND1-YL2
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
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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, Other, Nuclear, Receptors, Degraders, 7388, Tocris Bioscience
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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
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