BSJ-05-37

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

Structure

SERP Rating

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

No SERP comments found for BSJ-05-37