ND1-YL2

Name: ND1-YL2
Brand: Tocris Bioscience
SKU: 7388

Tocris Bioscience, part of Bio-Techne | Catalog # 7388

COA / SDS

SRC-1 peptide-based Degrader (PROTAC®); active in vivo

Key Product Details

Description:	SRC-1 peptide-based Degrader (PROTAC^®); active in vivo
Purity:	≥95% (HPLC)
Molecular Weight:	2385.93

View Full Technical Details for ND1-YL2

Technical Data
Citations

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 (K_i = 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
Single Letter 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 for ND1-YL2

Solubility

Soluble to 1mg/ml in water

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References for ND1-YL2

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

Lee Targeted degradation of transcription co-activator SRC-1 through the N-degron pathway. Angew.Chem.Int.Ed.