ND1-YL2

Pricing Availability   Qty
Description: SRC-1 peptide-based PROTAC®; active in vivo
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for ND1-YL2

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 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

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.

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

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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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