PF-04802367

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively[1].

Product Specifications

CAS Number

[1962178-27-3]

Product Name Alternative

PF-367

UNSPSC

12352005

Hazard Statement

H302

Target

GSK-3

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pf-04802367.html

Purity

98.43

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(C2=CC=C(OC)C(Cl)=C2)OC=N1)NCCCN3N=CN=C3

Molecular Formula

C16H16ClN5O3

Molecular Weight

361.78

Precautions

H302

References & Citations

[1]Steven H Liang, et al. Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging. Angew Chem Int Ed Engl. 2016 Aug 8;55 (33) :9601-5.|[2]Vadim Bernard-Gauthier, et al. Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery. J Med Chem. 2019 Nov 14;62 (21) :9600-9617.