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IQ-1S free acid

CAS No. : 23146-22-7

MCE 站：IQ-1S free acid

产品活性：IQ-1S free acid 是一种 NF-κB/激活蛋白1 (AP-1) 抑制剂，IC₅₀ 为 2.3±0.41 μM。IQ-1S free acid 对三种 JNK 都具有高的结合亲和力 (K_d 值)，对 JNK3，JNK1 和 JNK2 的 K_d 值分别为 100 nM，240 nM 和 360 nM。

研究领域：MAPK/ERK Pathway

作用靶点：JNK

In Vitro: Compound IQ-1S is a potent, noncytotoxic inhibitor of pro-inflammatory cytokine [interleukin (IL)-1α, IL-1β, IL-6, IL-10, tumor necrosis factor (TNF)-α, interferon-γ, and granulocyte-macrophage colony-stimulating factor] and nitric oxide production by human and murine monocyte/macrophages. The effect of IQ-1S is evaluated on LPS-induced cytokine production in human PBMCs. Among the 12 cytokines analyzed, LPS (200 ng/mL) consistently induces five (IL-1α, IL-1β, IL-6, IL-10, and TNF-α) in PBMCs compared with DMSO-treated control cells. Production of all of these cytokines is significantly inhibited by 20 μM IQ-1S. Among them, TNF-α production is inhibited completely by IQ-1 (>99%), the levels of IL-1α, IL-1β, and IL-10 are decreased by 85%, and IL-6 production is decreased by 33%.

In Vivo: When mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1S) i.p., the serum exposure of the compound is also good, with AUC_0-12h values of 2.9 and 7.4 μM/h, respectively.

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