BSJ-01-175

BSJ-01-175 : Covalent of CDK12 and CDK13

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe BSJ-01-175 is in the process of SERP review.

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Information

CDK12
CDK13

Covalent

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q9NYV4

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 156 nM

Potency Assay: Biochemical Activity

PDB ID for probe-target interaction (3D structure): 7NXK

Target aliases:

Cyclin-dependent kinase 12, KIAA0904, CRKRS, CRK7, ...

DOI Reference: 10.1016/j.ejmech.2021.113481

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: CDK7

Potency end-point : IC50 187 nM

Potency assay (off target): KiNativ profiling @ 1 uM of 270 Kinase, only shows >75% inhibition of CRK7/CDK12; CDK9: IC50 - 367 nM CDK2: IC50 - 4510 nM

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This probe contains an electrophilic warhead, and global proteomic conjugation studies are necessary before use of this probe (in vitro and in vivo) can be recommended. The study is also critically missing in vivo PD evaluation to allow assessing the PD/efficacy relationship. Without it, there is insufficient evidence that the tumor growth inhibitory effect is predominantly driven by CDK12/13 inhibition.

(last updated: 22 Dec 2022 )