GSK2334470

GSK2334470 : Type I Inhibitor of PDPK1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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Information

PDPK1

Type I Inhibitor

30 nM - 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O15530

Target Class: Protein kinase

Target SubClass: AGC

Potency: IC50

Potency Value: 2.5 nM

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

Target aliases:

3-phosphoinositide-dependent protein kinase 1, PDK ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): GSK2334470 was tested against a panel of 285 kinases and found to be >1,000-fold selective for PDK1, inhibiting only 24 kinases >50% at 10 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 21 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 8 Sept 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This compound is a potent and selective inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1). It has low nanomolar potency against the PDK1 enzyme. GSK2334470 appears selective based on the published data. It has been tested against 95 different protein kinases, and none of them were inhibited to a significant extent at a 1 uM screening concentration. In addition, GSK2334470 does not inhibit the 15 lipid kinases that were tested. In cells, GSK2334470 is active at concentrations between 30 nM and 1 uM, depending on the particular conditions and readout being measured. The authors demonstrate, for example, inhibition of the phosphorylation of SGK1, SGK2, SGK3, P70S6K, and AKT in cells in certain contexts. No pharmacokinetic data was reported, so suitability for in vivo experiments is unknown.

(last updated: 19 Jun 2017 )