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100 mg | Get quote | |
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500 mg | Get quote | |
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Cat. No. : | HY-100233A |
M.Wt: | 270.24 |
Formula: | C15H9N3NaO+ |
Purity: | >98 % |
Solubility: |
IQ-1S is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 1.8±0.3 μM. IQ-1 has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 87 nM, 360 nM, and 390 nM for JNK3, JNK2, and JNK1, respectively. IC50 & Target: IC50: 1.8±0.3 μM (NF-κB/AP-1)[1] Kd: 87 nM (JNK3), 360 nM (JNK2), 390 nM (JNK1), 1.2 μM (PI3Kγ), 1.4 μM (CK1δ), 1.8 μM(MKNK2)[1] In Vitro: IQ-1S (The sodium salt of IQ-1) 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-1 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-1. 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%. IQ-1S inhibits LPS-induced TNF-α and IL-6 production in MonoMac-6 cells with IC50 values of 0.25 and 0.61 μM, respectively[1]. In Vivo: When mice are dosed with 12.5 and 30 mg/kg IQ-1S (The sodium salt of IQ-1) i.p., the serum exposure of the compound is also good, with AUC0-12h values of 2.9 and 7.4 μM/h, respectively[1].
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