NK7-902

NK7-902 : Molecular Glue of NEK7

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe NK7-902 is in the process of SERP review.

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Information

NEK7

Molecular Glue

1 µM

In Vitro Validations

Uniprot ID: Q8TDX7

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: Kd

Potency Value: 1160 nM

Potency Assay: SPR of ternary complex formation

PDB ID for probe-target interaction (3D structure): 9H59

Target aliases:

Serine/threonine-protein kinase Nek7, NEK7, NEK7_H ...

DOI Reference: 10.1016/j.chembiol.2025.06.005

Uniprot ID: Q8TDX7

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: Kd

Potency Value: 49 nM

Potency Assay: SPR of binary complex

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

Target aliases:

Serine/threonine-protein kinase Nek7, NEK7, NEK7_H ...

DOI Reference: 10.1016/j.chembiol.2025.06.005

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): Selectivity of NK7-902 was assessed by mass spectrometry-based proteomics analysis of human primary monocytes following an 18 h treatment with 1 μM. NEK7 was the most significantly down-regulated protein across all quantified proteins while NEK6, the protein most homologous to NEK7 (86% identical in their catalytic domain) does not contain a β-hairpin and was not degraded by NK7-902.

Potency assay, off target (cells): Expression proteomics analysis of NK7-902 was also done in human iPS cells which express Sal-like protein 4 (SALL4). NEK7 was the most strongly and significantly decreased protein in iPS cells and SALL4 protein levels were detected but unchanged after treatment with NK7-902. A significant down-regulation of SALL3 , another member of the SALL gene family was observed. FLT3 interacting zinc finger 1 (FIZ1) and the zinc finger transcription factor IKZF4 were also significantly down-regulated by NK7-902 in human iPS cells.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

NK7-902 is a valuable chemical probe (degrader) to study NEK7-mediated NLRP3 biology. In contrast to other tool compounds NK7-902 not only degrades human and NHP but also mouse protein. In addition, its oral bioavailability allows studies in vivo. The good selectivity was confirmed in a proteomics analysis in human primary monocytes.

(last updated: 1 Sept 2025 )