ARD-266

Degrader (PROTAC) of AR

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ARD-266 is in the process of SERP review.

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Information

Degrader (PROTAC)

10-100 nM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

ARD-266 potently induces cellular degradation of Androgen receptor at nanomolar concentrations within three hours of treatment in several tested human cell lines. As expected, degradation resulted in downregulation of Androgen receptor target genes. Effects of ARD-266 were prevented by pretreatment of cells with an AR antagonist, a VHL ligand or inhibitors of an E1 enzyme or the proteasome, suggesting that AR-266 is a true PROTAC degrader of Androgen receptor. Proteome-wide selectivity of ARD-266 has not been established and this limits the utility of this probe as a general tool to study Androgen receptor-specific downregulation.

(last updated: 18 Feb 2021 )