MSC2530818

MSC2530818 : Inhibitor of CDK8, CDK19

Structure

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Information

CDK8
CDK19

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P49336

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 2.6 ± 0.1 nM

Potency Assay: FRET-based Lanthascreen binding competition assay

PDB ID for probe-target interaction (3D structure): 5IDN

Target aliases:

Cyclin-dependent kinase 8, CDK8, CDK8_HUMAN, Prote ...

DOI Reference: 10.1021/acs.jmedchem.6b00597

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Minimal activity in the CEREP panel, being active on the dopamine transporter (IC50 = 8.5 μM) as the only activity below 10 μM, and demonstrated minimal hERG inhibition (18%@10 μM).

Potency assay (off target): Testing against a 264 kinase panel gave inhibition of only a single kinase by more than 50% at 1 μM (GSK3α IC50 = 691 nM).

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