SK2188

SK2188 : Degrader (PROTAC) of AURKA

Structure

SERP Rating

Probe SK2188 is in the process of SERP review.

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Information

AURKA

Degrader (PROTAC)

up to 500 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): SK2188 was assessed against a panel of 468 kinases via a discoverX KINOMEscan @ 100 and 1000 nM.

Probe Selectivity in Vitro:

At 1000 nM, besides AURKA (0.3% control), SK2188 only binds 15 other kinases with a value < 35% control (standard cut-off value). At 100 nM only AURKA and TrkA were bound, indicating excellent target binding selectivity.

Potency assay, off target (cells): Mass spectrometry-based shotgun proteome profiling was used to assess the degradation in cellular environment.

Probe Selectivity in Cell:

From a total of 7175 detected proteins, AURKA was the most significantly downregulated at both 100 nM (-log10 p = 11.8, log2FC = −2.0) and 1000 nM (-log10 p = 4.3, log2FC = −2.0). Cumulatively at both concentrations tested, there are only 8 other differentially expressed proteins, however at a much lower significance (-log10 p < 2.5).

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