THAL-SNS-032

Degrader (PROTAC) of CDK9, CDK10

Structure

Information

Protein target names: CDK9, CDK10

Mechanism of action: Degrader (PROTAC)

Recommended in-cell concentration:
250 - 1000 nM

In Vitro Validations

Uniprot ID: P50750
Target Class: Kinase
Target SubClass: CMGC
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: no
Target aliases:
Cyclin-dependent kinase 9, TAK, CDC2L4, CDK9, CDK9 ...

DOI Reference: 10.1038/nchembio.2538

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating

(last updated: 13 Mar 2021 )

SERP Ratings

In Cell Rating

SERP Comments:

This probe is a degrader version of the inhibitor NVP-2.  Both probes inhibit additional kinases in vitro, but the probe here selectively degrades CDK9 (and CDK10).  Best use would be comparison of the effects due to loss of CDK9 (and CDK10) versus inhibition of these kinases.  Probe has been used in the MOLT4 cell line, use of this probe in additional cell lines would need initial validation of the degradation efficiency.

(last updated: 19 Mar 2021 )

SERP Ratings

In Cell Rating

SERP Comments:

A potential and selective PROTAC molecule to degrade cellular level of CDK9. Very fast degradation kinetics was observed. Good evidence of UPS mediated degradation using CRBN negative cell line control. DC50 of this particular probe was not determined and the relevant concentration to effectively degrade CDK9 can be lower. Global degradation selectivity might be different as short time point (2h) was used in the MS experiment.

(last updated: 29 Mar 2021 )