GSK256066

Protein target name:

PDE4B

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

0.1-1 nM

Probe Availability

MedChemExpress

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

Nucleic acid metabolism

Subclass:

Phosphodiesterase

HUGO ID:

HGNC:8781

Entrez gene ID:

5142

UNIPROT ID:

Q07343

Target alias:

DPDE4, PDEIVB, phosphodiesterase 4B

Probe Details

Chemical Probes Portal ID:

CPP2218

Probe alias:

GSK256066, O66

PubChem CID:

9827968

ChEMBL ID:

CHEMBL570015

SMILES string:

O=C(N)C1=C(C2=CC(S(=O)(C3=CC=CC(C(N(C)C)=O)=C3)=O)=CC(C)=C2N=C1)NC4=CC=CC(OC)=C4

InChi Key:

JFHROPTYMMSOLG-UHFFFAOYSA-N

Control compound:

cpd 3

Orthogonal probe:

R(-)Rolipram

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

pIC50

11.1

Potency assay:

Scintillation Proximity Assay (SPA)

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

3GWT

Structure-activity relationship:

yes

Off target activity

Probe Selectivity in Vitro:

>1000-fold selective versus PDEs 1–3 and 5–7

In cell validation

On target activity in cells

Potency in cells:

pIC50

11 (LPS)9.9 (Whole Blood)

Potency assay (cells):

Inhibition of LPS induced TNF-α production from isolated human peripheral blood mononuclear cells (PBMC) or human whole blood using IGEN technology

In vivo validation

Organism:

Rat

Dose:

1 mg/Kg

Route of delivery:

OralIntravenous

Plasma half life:

1.1 h (IV)

Systemic clearance:

39 mL/min/kg

Primary Reference

Reference (doi):

10.1124/jpet.110.173690 10.1016/j.bmcl.2009.04.012

Reference (PMID):

21205923 19656678

GSK256066

Probe Availability

Probe Information

Target Details

DPDE4, PDEIVB, phosphodiesterase 4B

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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GSK256066

Probe Availability

Probe Information

Target Details

DPDE4, PDEIVB, phosphodiesterase 4B

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?