AKR1C3-PROTAC-5

AKR1C3-PROTAC-5 : Degrader (PROTAC) of AKR1C3 and AR

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe AKR1C3-PROTAC-5 is in the process of SERP review.

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Information

AKR1C3
AR (Other variant:splicing variant 7)

Degrader (PROTAC)

10 nM, up to 100 nM

Probe Availability:

ProbeChem

In Vitro Validations

Uniprot ID: P42330

Target Class: Enzyme

Target SubClass: Reductase

Potency: IC50

Potency Value: 77.7 nM

Potency Assay: Enzymatic assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Aldo-keto reductase family 1 member C3, KIAA0119, ...

DOI Reference: 10.1038/s42004-024-01177-4

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): PROTAC 5 provided a trend of degradation of AKR1C1/C2 in a time-dependent manner, but to a lesser extent than AKR1C3, with AKR1C1/C2 DC50 = 49 nM

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Results from this can be used as orthogonal tool to validate with more specific genetic knockdown approaches, but cellular selectivity data and/or proteomic data are missing.

(last updated: 31 Oct 2024 )