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JAK-IN-23

CAS No. :

MCE 站：JAK-IN-23

产品活性：JAK-IN-23 是 JAK/STAT 和 NF-κB 的双重抑制剂，具有口服活性。JAK-IN-23 对J AK1/2/3 具有抑制作用，IC₅₀ 值分别为 8.9 nM、15 nM 和 46.2 nM。JAK-IN-23 对干扰素刺激基因 (ISG) 和 NF-κB 通路具有较强的抑制活性，IC₅₀ 值分别为 3.3 nM 和 150.7 nM。JAK-IN-23 具有很强的抗炎作用，可以减少各种促炎因子的释放。JAK-IN-23 可用于炎症性肠病 (IBD) 的研究。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling  |  Immunology/Inflammation  |  NF-κB

作用靶点：JAK  |  STING  |  NF-κB  |  STAT

In Vitro: JAK-IN-23 inhibits JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM ａnd 46.2 nM, respectively.
JAK-IN-23 shows potent inhibitory activities against ISG ａnd NF-KB with IC₅₀ values of 3.3 nM ａnd 150.7 nM, respectively.
WB－－- JAK-IN-23 (0.33μM, 1μM, 3μM; 24 h) can simultaneously block JAK-STAT1/3 ａnd NF-κB proinflammatory signaling pathways in THP1-dual cells.
JAK-IN-23 (0.003-3 μM; 24 h) decreases the release of various proinflammatory factors, including IL-6, IL-8, IL-1β in THP1-dual cells stimulated by LPS.
JAK-IN-23 (0.11-3 μM; 24 h) decreases the release of various proinflammatory factors, including TNF-α, IL-12, IL-10 ａnd IFNγ in LPS-induced peripheral blood mononuclear cells (PBMCs).
JAK-IN-23 (1 μM) inhibits the expression of a variety of inflammation-related genes induced by LPS, including IL-1B, TNF, IL12B, ａnd IL-23A ａnd has inhibitory effects on the expression of genes involved in the unfolded protein response that was induced by LPS (1 μg/mL).

In Vivo: JAK-IN-23 (1-5 mg/kg, oral) produces a strong anti-inflammatory activity in both dextran sulfate sodium (DSS) - ａnd 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced acute enteritis models ａnd restores the structural composition of gut microbiota.

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