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PF-04802367

CAS No. : 1962178-27-3

MCE 站：PF-04802367

产品活性：PF-04802367 (PF-367) 是一种高选择性 GSK-3 抑制剂，对 GSK-3β 酶的 IC₅₀ 为 2.1 nM。PF-04802367 具有理想的中枢神经系统 (CNS) 特性和效力。PF-04802367 抑制两种 GSK-3 亚型（GSK-3α 和 GSK-3β）效果差不多， IC₅₀ 值分别为 10.0 和 9.0 nM。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：GSK-3

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.
PF-367 has reasonable?in vitro?stability in human hepatic microsomes (t_1/2=78.7 min), has excellent passive permeability.
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.
PF-367 has good cell viability (IC₅₀?of 117 μM in THLE cytotoxicity assays) and an IC₅₀?>100 μM in a hERG screening assay.
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.

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.
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.

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