PF-04802367 NEW
| Price | $44 | $107 | $163 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PF-04802367 | CAS No.: 1962178-27-3 |
| Purity: 98.76% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PF-04802367 |
| 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. |
| In vitro | PF-04802367 (PF-367) effectively inhibits GSK-3β enzymatic activity in vitro, with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively [1]. It exhibits reasonable in vitro stability in human hepatic microsomes (t1/2=78.7 min) and has excellent passive permeability [1]. In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibits phosphorylation of tau with an IC50 of 466 nM [1]. PF-367 demonstrates good cell viability (IC50 of 117 μM in THLE cytotoxicity assays) and an IC50 >100 μM in a hERG screening assay [1]. It shows significant right shifts against β-catenin translocation in HeLa cells with an EC50 of 6.2 μM, gene transcription in U2OS cells with an EC50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with an EC50 of 9.0 μM [1]. |
| In vivo | PF-04802367 (PF-367) is a potent type-I dual GSK-3α/β inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. It demonstrates dose-dependent inhibition of tau phosphorylation in the brain at subcutaneous doses of 1, 3.2, 10, 32, or 50 mg/kg. Additionally, PF-367 exhibits promising ADME properties, and robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (276.41 mM), Sonication is recommended. |
| Keywords | PF367 | PF-04802367 | PF 367 | protein | PF 04802367 | disease | Alzheimer | PF-367 | Glycogen synthase kinase-3 | kinase-3 | synthase | Inhibitor | phosphorylation | neurology | GSK-3 | neurodegenerative | tau | Glycogen synthase kinase 3 | inhibit | Glycogen | PF04802367 |
| Inhibitors Related | PHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | CHIR-99021 HCl | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone |
| Related Compound Libraries | Highly Selective Inhibitor Library | Glycolysis Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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