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Pyridone 6

CAS No. : 457081-03-7

MCE 站：Pyridone 6

产品活性：Pyridone 6 是一种 pan-JAK 抑制剂，有效抑制 JAK 激酶家族，作用于 JAK2，TYK2，JAK3 和 JAK1，IC₅₀ 分别为 1 nM，1 nM，5 nM 和 15 nM。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: Pyridone 6 is tested as an inhibitor of 21 other protein kinases; Pyridone 6 inhibits these kinases with IC₅₀s ranging from 130 nM to >10 μM. Pyridone 6 inhibits IL2 driven proliferation of CTLL cells with IC₅₀=0.1 μM and IL4 driven proliferation with IC₅₀=0.052 μM. Pyridone 6 (P6) is shown to inhibit kinase by interacting within the ATP-binding cleft of each JAK. The IC₅₀ of Pyridone 6 is 3 nM for all of these cytokines; this is comparable to the reported IC₅₀s of Pyridone 6 for JAK2, Tyk2, and JAK3. Pyridone 6 strongly inhibits Th2 and modestly inhibits Th1, whereas it enhances Th17 development when present within a certain range of concentrations. Pyridone 6 reduces IFN-γ and IL-13, whereas it enhances IL-17 and IL-22 expression. Pyridone 6 also inhibits both Th1 and Th2 development, whereas it promotes Th17 differentiation from naive T cells when present within a certain range of concentrations.

In Vivo: Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty polylactic acid with glycolic acid (PLGA) nanoparticles (C-nano) seemed to have no effect.

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