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Submit ReviewND1-YL2
说明： SRC-1 peptide-based Degrader (PROTAC®); active in vivo
纯度： ≥95% (HPLC)
生物活性 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.
许可信息
Sold under license from Pohang University of Science and Technology
技术数据 for ND1-YL2
| 分子量 | 2385.93 |
| 公式 | C114H189N27O28 |
| 序列 |
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 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for ND1-YL2
| 溶解性 | Soluble to 1 mg/ml in water |
产品说明书 for ND1-YL2
参考文献 for ND1-YL2
参考文献是支持产品生物活性的出版物。
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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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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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