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  3. PF-04802367

PF-04802367 (Synonyms: PF-367)

Cat. No.: HY-122026
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-04802367 Chemical Structure

PF-04802367 Chemical Structure

CAS No. : 1962178-27-3

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5 mg USD 380 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
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25 mg USD 1150 In-stock
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100 mg USD 2850 In-stock
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Description

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].

IC50 & Target[1]

GSK-3α

10 nM (IC50)

GSK-3β

9 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats[1]
Dosage: 1, 3.2, 10, 32 or 50 mg/kg
Administration: A single subcutaneous
Result: Inhibition of phosphorylation of tau in brain is dose-dependent.
Molecular Weight

361.78

Formula

C₁₆H₁₆ClN₅O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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PF-04802367
Cat. No.:
HY-122026
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