ABEMACICLIB

ABEMACICLIB : ATP competitive inhibitor of CDK4, CDK6

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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 ABEMACICLIB is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CDK4
CDK6

competitive ATP inhibitor

up to 2 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P11802

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 2 nM

Potency Assay: radiometric-filter binding assay

PDB ID for probe-target interaction (3D structure): 7SJ3, 5L2S, 7O7K, 7O7J

Target aliases:

Cyclin-dependent kinase 4, CDK4, CDK4_HUMAN, PSK-J ...

DOI Reference: 10.1007/s10637-014-0120-7

Uniprot ID: P11802

Target Class: Kinase

Target SubClass: CMGC

Potency: Ki

Potency Value: 0.6 nM

Potency Assay: radiometric-filter binding assay

PDB ID for probe-target interaction (3D structure): 7SJ3, 5L2S, 7O7K, 7O7J

Target aliases:

Cyclin-dependent kinase 4, CDK4, CDK4_HUMAN, PSK-J ...

DOI Reference: 10.1007/s10637-014-0120-7

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity was evaluated in a panel of 100 protein kinases (Millipore/UBI). Profiled against 456 kinases (KINOMEscan, DiscoverRx) for single point binding at 200 nM and 2 μM concentrations: at 2 uM shows a binding profile significantly concentrated in the CGMC family of kinases that comprises cyclin-dependent kinases and MAPK kinases.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This probe is of high quality and has good selectivity for its target. However, at concentrations below the recommended there are issues with in-family selectivity which may make making conclusions more complex given the linked phenotype. A non-active probe control would also have been useful for here. Overall, this is a nicely designed probe that can be used to interrogate the target.

(last updated: 22 Jun 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Abemaciclib is a potent inhibitor of many CDKs as well as many CMGC family member such as DYRK1A and HIP kinases. It would be not be possible to assign a function in cells to CDK4/6 based on Abemaciclib alone. Orthogonal approaches or probes and dose-response data may be required.

(last updated: 17 Jul 2023 )