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Tocris Bioscience™ ND1-YL2

SRC-1 peptide-based PROTAC™; active in vivo

Supplier:  Tocris Bioscience™ 7388/100U

Catalog No. 7388100U


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Description

Description

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.

Specifications

Specifications

95%
Store at -20°C
M.W.-observed: 2385.93
100 μg
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