YKL-01-116

YKL-01-116 : Covalent inhibitor of CDK7

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 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 YKL-01-116 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CDK7

Covalent

up to 5 uM

Probe Availability:

MedKoo

In Vitro Validations

Uniprot ID: P50613

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 7.6 nM

Potency Assay: Biochemical Radioactivity Assay

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

Target aliases:

Cyclin-dependent kinase 7, STK1, MO15, CDKN7, CAK1 ...

DOI Reference: 10.1016/j.celrep.2017.09.056

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): KiNativ profiling assay in Jurkat cells @ 1 µM Very selective within CDK family. Off targets detected: CDK9: IC50 > 1 µM; CDK2: IC50 = 1.1 µM; CHK2: IC50 = 7.4 nM; FGR: IC50 = 5.1 nM; HIP4K: IC50 = 178 nM; PRKCQ: IC50 = 4.9 nM; RET: IC50 = 63.5 nM; SRC: IC50 = 3.9 nM

Probe Selectivity in Vitro:

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Potential off-target inhibition of CHK2 may confound interpretation of results.

(last updated: 14 Apr 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Some additional off-targets have been seen @1 µM. In addition, there is another chemical tool for CDK7, which can be used as control: JNJ-3738 https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/JNJ-3738.

(last updated: 23 Sept 2024 )