DYR684

DYR684 : Degrader (PROTAC) of DYRK1A and DYRK1B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe DYR684 is in the process of SERP review.

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Information

DYRK1A
DYRK1B

Degrader (PROTAC)

100 nM, up to 300 nM

Probe Availability:

MedChemExpress

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KinomeScan of DYR684 at 1 μM reveals that DYR684 targets 11 out of 468 kinases (S(35) score 0.024).

Potency assay, off target (cells): Unbiased quantitative global proteomic profiling was used to assess selectivity in cell. Over 6500 proteins were quantified in the cell lysates of either HEK293 or SH-SY5Y neuroblastoma cells after treatment with 100 nM DYR684 or vehicle for 24 h. DYRK1A was the only protein kinase that was found to be significantly degraded upon treatment. DCAF7 levels were not affected in response to DYR684. Overall, very few proteins showed significant changes upon treatment, including two zinc finger proteins (WIZ and ZFP91) that have previously been identified as lenalidomide- or pomalidomide-dependent neo-substrates of CRBN.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

DYR684 is a very well characterized degrader of DYRK1A and DYRK1B. It is a very good probe for cellular studies as it can be used at moderate nanomolar concentrations and showed good selectivity in an unbiased proteomics experiment. It may also be a good in vivo probe on the basis of a PK study, but users should keep in mind that no in vivo degradation data was presented in the manuscript.

(last updated: 25 Oct 2024 )