S84566 |
IQ-1S (free acid) |
| 源叶(MedMol) | 98% |
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- 产品描述： IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
- 靶点： JNK3:100 nM (Kd);JNK1:240 nM (Kd);JNK2:360 nM (Kd);CK1δ:0.38 μM (Kd);PI3Kγ:0.47 μM (Kd);MKNK2:0.92 μM (Kd)
- 体外研究：
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%
- 体内研究：
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 AUC0-12h values of 2.9 and 7.4 μM/h, respectively
- 参考文献：
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.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 4.044 ml 20.222 ml 40.445 ml 5 mM 0.809 ml 4.044 ml 8.089 ml 10 mM 0.404 ml 2.022 ml 4.044 ml 50 mM 0.081 ml 0.404 ml 0.809 ml
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