BSJ-05-37

BSJ-05-37 : Degrader (PROTAC) of ITK

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe BSJ-05-37 is in the process of SERP review.

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Information

Degrader (PROTAC)

250 nM, up to 1 uM

In Vitro Validations

Uniprot ID: Q08881

Target Class: Kinase

Target SubClass: Tyr kinase

Potency: Inhibition

Potency Value: 97%

Potency Assay: KinomeSCAN

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

Target aliases:

Tyrosine-protein kinase ITK/TSK, LYK, EMT, ITK, IT ...

DOI Reference: 10.1016/j.chembiol.2023.03.007

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Biochemical selectivity of BSJ-05-037 was assessed against a panel of 468 kinases with a treatment concentration of 1 μM (KINOMEscan), and found that only ITK, TRKA and MUSK scored with >90% inhibition.

Potency assay, off target (cells): Protein abundance measurements were made using tandem mass tag quantitative mass spectrometry on MOLLT4 cells treated with 100 nM BSJ-05-37 for 5 h.

Probe Selectivity in Cell:

These data identified significant downregulation of ITK, as well as RNF166, ZNF653, and ZNF692.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

We recommend this probe for use in cells, as long as the reported off-targets are considered during experimental design. The concentration at which the probe is used should be considered, as inhibition of other kinases (TRKA and MUSK) has been reported at higher concentrations. Additionally, transcription factor degradation (RNF166, ZNF653, and ZNF692) was observed by proteomics, which can influence the observed phenotype. We suggest considering orthogonal experiments to validate that potential off-targets are not responsible for a given phenotype. Regarding in vivo use, the fraction unbound has not been reported, which would be beneficial to know to establish the required dose to ensure sufficient unbound exposure and avoid potential off-target effects.

(last updated: 6 Feb 2026 )