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PF-04802367

Catalog No. T9611   CAS 1962178-27-3

PF-04802367 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. It shows desirable central nervous system (CNS) properties and potency. It 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.

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PF-04802367 Chemical Structure
PF-04802367, CAS 1962178-27-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 87.00
5 mg In stock $ 213.00
10 mg In stock $ 347.00
25 mg In stock $ 589.00
50 mg In stock $ 842.00
100 mg In stock $ 1,160.00
500 mg In stock $ 2,330.00
1 mL * 10 mM (in DMSO) In stock $ 235.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-04802367 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. It shows desirable central nervous system (CNS) properties and potency. It 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.
Targets&IC50 GSK-3β:9 nM (IC50), GSK-3α:10 nM (IC50)
In vitro PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively[1].
PF-367 has reasonable in vitro stability in human hepatic microsomes (t1/2=78.7 min), has excellent passive permeability[1].
In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC50 of 466 nM[1].
PF-367 has good cell viability (IC50 of 117 μM in THLE cytotoxicity assays) and an IC50 >100 μM in a hERG screening assay[1].
PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC50 of 6.2 μM, gene transcription in U20S cells with EC50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC50 of 9.0 μM[1].
In vivo PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent[1].
PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo[2].
Molecular Weight 361.78
Formula C16H16ClN5O3
CAS No. 1962178-27-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (276.41 mM), sonification is recommended.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Compound Library Anti-Ovarian Cancer Compound Library Bioactive Compound Library Anti-Cancer Metabolism Compound Library Anti-Lung Cancer Compound Library Kinase Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Neuronal Differentiation Compound Library

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Keywords

PF-04802367 1962178-27-3 PI3K/Akt/mTOR signaling Stem Cells GSK-3 PF367 PF 367 protein PF 04802367 disease Alzheimer PF-367 Glycogen synthase kinase-3 kinase-3 synthase Inhibitor phosphorylation neurology neurodegenerative tau Glycogen synthase kinase 3 inhibit Glycogen PF04802367 inhibitor

 

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