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Pyridone 6

CAS No. : 457081-03-7

MCE 国际站：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  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

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.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Anti-Liver Cancer Compound Library   |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Pain-Related Compound Library  |  JAK-IN-20  |  JAK1-IN-9  |  AT9283  |  RO495  |  TK4b  |  JAK-IN-17  |  (E/Z)-Zotiraciclib  |  JAK-IN-10  |  (3R,4S)-Tofacitinib  |  JAK3/BTK-IN-6  |  Tyk2-IN-5  |  Brevilin A  |  Broussonin E  |  Itacnosertib  |  RO8191  |  Axltide  |  Fosifidancitinib  |  JAK3-IN-6  |  Upadacitinib  |  JAK-IN-24  |  AZD-1480  |  Baricitinib-d₃  |  Tofacitinib-¹³C₃  |  AZ-3  |  Delphinidin chloride  |  TK4g  |  Tofacitinib Prodrug-1

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