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。

IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC 50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (K d values) in the nanomolar range for all three JNKs with K d s of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.

Solid

JNK3 100 nM (Kd) JNK1 240 nM (Kd)

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%. has not independently confirmed the ac

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Schepetkin IA, et al. Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol. 2012 Jun;81(6):832-45.

In Vitro: DMSO : 16.67 mg/mL (67.42 mM; Need ultrasonic)配制储备液